Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

10202564 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
3217 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
CHEMBL362628 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
10202564 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
3217 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
CHEMBL362628 1524 14 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
6918836 60541 16 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
CHEMBL175835 60541 16 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
6918836 60541 16 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
CHEMBL175835 60541 16 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
16718917 181682 0 None 2290 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 181682 0 None 2290 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
16718920 189677 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
CHEMBL515307 189677 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
71459954 79182 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
CHEMBL2113386 79182 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
71459954 79182 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 79182 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
11234629 202213 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL609741 202213 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
16112801 181091 0 None 1258 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL476006 181091 0 None 1258 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
11463428 201752 0 None - 1 Human 9.0 pEC50 = 9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606639 201752 0 None - 1 Human 9.0 pEC50 = 9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
11200511 201730 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 201730 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
11280663 202244 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
CHEMBL609995 202244 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
11223004 202214 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 202214 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
11749539 202241 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
CHEMBL609992 202241 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
11451904 202295 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL610254 202295 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11210467 202209 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
CHEMBL609737 202209 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
11384146 201733 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 201733 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
44403084 71744 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196622 71744 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
23655289 88689 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL235986 88689 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
45484384 198867 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584049 198867 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
3245407 48105 25 None 1 5 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 48105 25 None 1 5 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
45484333 196816 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565724 196816 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
46880707 8538 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1094370 8538 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
11333554 96661 22 None -64 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96661 22 None -64 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
25208878 181063 0 None 77 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL475969 181063 0 None 77 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
23655287 88688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
CHEMBL235985 88688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
10067306 198866 0 None 8 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 198866 0 None 8 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
45484307 196829 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565753 196829 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403055 69847 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193824 69847 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435607 89137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236576 89137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
22028185 199040 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585931 199040 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435608 89140 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236577 89140 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435643 147599 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393107 147599 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23655462 90223 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL238277 90223 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
10017687 67281 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL188182 67281 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
10472158 196825 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 196825 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
11775364 201787 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 201787 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
23655468 89391 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236989 89391 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
14571158 149081 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL394303 149081 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
11211722 201735 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606558 201735 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
73354882 89693 1 None 14 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89693 1 None 14 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11363934 202243 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
CHEMBL609994 202243 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
11453792 201731 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606548 201731 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
45484381 198489 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
CHEMBL577687 198489 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
46880531 6299 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081793 6299 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
44435614 154450 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL399013 154450 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
73356442 89696 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376485 89696 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44435616 147854 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393312 147854 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9902533 133602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
CHEMBL371292 133602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
45484297 197296 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568672 197296 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44433197 88775 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236313 88775 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11709684 198617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
CHEMBL578826 198617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
11709684 198617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL578826 198617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403064 133572 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371132 133572 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10380133 198336 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL576315 198336 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435635 89202 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236772 89202 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435604 154861 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL400627 154861 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484398 196867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565977 196867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435646 145560 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL391517 145560 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16718827 175409 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
CHEMBL457570 175409 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
11385064 201734 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606557 201734 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44435629 148694 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393997 148694 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484352 198636 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL579063 198636 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435641 147597 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393106 147597 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9999118 6169 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081094 6169 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
45484299 197217 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568249 197217 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45484322 198805 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL583389 198805 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
73351903 89695 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89695 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89698 0 None 32 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89698 0 None 32 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44433198 147113 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392746 147113 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403072 70409 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194568 70409 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435610 88795 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236404 88795 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484399 198964 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585098 198964 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133602 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133602 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
12147013 65582 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL183203 65582 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
46880657 6379 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082198 6379 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
44435647 88509 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235117 88509 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880655 5552 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1076684 5552 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
11316594 202242 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
CHEMBL609993 202242 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
46227395 200129 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL596199 200129 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11351089 201736 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606559 201736 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
11440676 202215 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
CHEMBL609743 202215 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
44435637 89364 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236976 89364 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
5 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5202 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
CHEMBL39 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
DB08839 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 139 72 None -181 26 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
44435627 88500 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235070 88500 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484382 196817 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
CHEMBL565730 196817 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
44435638 154928 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL401018 154928 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11200157 201763 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606705 201763 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
73347306 89694 0 None 15 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89694 0 None 15 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11452988 202240 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
CHEMBL609991 202240 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
44435653 147400 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392976 147400 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435628 148502 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393830 148502 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10407367 196793 0 None 10 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 196793 0 None 10 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44403059 124373 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363827 124373 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435613 154403 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398809 154403 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
23655469 89392 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236990 89392 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
46880486 6170 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081095 6170 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10199819 133608 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371318 133608 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
46880607 5974 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079977 5974 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
10150497 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
3240 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
CHEMBL392760 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
10150497 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
10150497 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
3240 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
CHEMBL392760 4074 47 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
73350387 89697 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89697 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
9840311 5550 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076665 5550 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
44435642 88637 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235734 88637 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11725505 199039 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585930 199039 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44433196 88722 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236104 88722 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10177537 124376 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363843 124376 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435649 145825 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL391713 145825 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23625764 147305 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL392899 147305 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880608 6020 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080316 6020 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10337743 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
8429 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
CHEMBL571858 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
10337743 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 4076 18 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
44435652 89254 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236812 89254 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435639 88548 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235306 88548 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880529 6171 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
CHEMBL1081110 6171 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
21071574 124083 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL363275 124083 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
44433193 88721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236103 88721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10042892 5532 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076583 5532 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
45484383 196818 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565731 196818 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
44403096 72128 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
CHEMBL197845 72128 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
23655465 89388 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL236987 89388 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
44435650 88510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235118 88510 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
11361090 64305 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181066 64305 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
11624561 70287 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL187865 70287 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL194307 70287 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44389001 63801 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180221 63801 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
11396708 202211 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
CHEMBL609739 202211 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
11524473 134839 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL371886 134839 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
11739679 169852 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL444015 169852 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
44403044 161711 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL413525 161711 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
11282884 202297 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
CHEMBL610256 202297 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
44389081 62653 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178385 62653 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
49836923 18763 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277918 18763 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554395 18723 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18723 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
11201726 202300 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
CHEMBL610259 202300 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
49836825 18722 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
CHEMBL1277564 18722 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
49836826 18732 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277656 18732 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44389004 123126 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL361180 123126 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
49836827 18741 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277751 18741 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836828 18749 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277836 18749 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554394 18733 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277657 18733 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44433195 146885 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392541 146885 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263302 191984 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191984 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
46189984 68890 1 None - 1 Human 8.0 pIC50 = 8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68890 1 None - 1 Human 8.0 pIC50 = 8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
11316095 201788 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606817 201788 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
162676953 183522 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4799851 183522 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
24784575 176714 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
CHEMBL459989 176714 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
21071390 1987 53 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
8689 1987 53 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
CHEMBL3286580 1987 53 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
DB11957 1987 53 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
18590409 10654 9 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170463 10654 9 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
46224917 199471 5 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591570 199471 5 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
49836615 18788 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1278091 18788 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
52918031 57666 4 None - 1 Human 7.0 pIC50 = 7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57666 4 None - 1 Human 7.0 pIC50 = 7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
24763349 62630 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783608 62630 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
16070169 60095 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642850 60095 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739214 60095 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53320775 60129 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642878 60129 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739546 60129 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
58357671 129036 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670291 129036 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
54582939 62721 6 None -8 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783957 62721 6 None -8 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901255 10955 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173281 10955 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
24783809 176713 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459988 176713 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
16019451 10989 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173570 10989 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
44126270 199151 6 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589389 199151 6 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
54585846 62727 5 None -38 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
CHEMBL1783963 62727 5 None -38 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
46880606 5973 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1079976 5973 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
46880756 6027 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080380 6027 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10136185 127179 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365753 127179 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
20901273 10641 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170291 10641 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
24763430 62619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783582 62619 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
49836617 18804 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278180 18804 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
18560541 10935 10 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173061 10935 10 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512797 142856 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3893286 142856 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
44435625 148998 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL394233 148998 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
25263297 184337 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 184337 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
4106 2502 22 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2502 22 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2502 22 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2502 22 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
44403048 132705 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL369910 132705 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
44388950 122604 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL360234 122604 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
46189932 68885 4 None - 1 Human 8.0 pIC50 = 8.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68885 4 None - 1 Human 8.0 pIC50 = 8.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53259021 69747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
16019576 10897 6 None 1995 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10897 6 None 1995 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
18591269 10967 2 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173362 10967 2 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10115005 71684 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196466 71684 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10117854 127425 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL366012 127425 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
18560059 10909 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172791 10909 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18559283 10655 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170464 10655 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
53324933 57622 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668502 57622 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
49836621 18655 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276926 18655 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
44403047 168428 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL434932 168428 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
16019286 10948 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173206 10948 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
46225001 199116 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589149 199116 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
18560559 10681 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170682 10681 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16804502 10685 13 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170686 10685 13 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18560180 10635 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170276 10635 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
197033 199152 64 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 199152 64 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
24783550 176732 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460194 176732 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
16019548 10882 10 None 23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172597 10882 10 None 23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
44156502 60984 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762569 60984 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
16117278 60149 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642884 60149 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739659 60149 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18590273 10777 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171632 10777 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117151 60087 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 60087 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 60087 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
56655504 68869 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68869 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849579 68874 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922619 68874 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357768 129038 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670293 129038 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
25123014 200431 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 200431 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44435624 89103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236541 89103 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24784573 176188 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459348 176188 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
49798859 10567 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169724 10567 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
7185128 10975 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173433 10975 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901271 10659 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170472 10659 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
20901291 10762 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1171486 10762 6 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
16019607 10928 3 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173005 10928 3 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901207 10984 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10984 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
10202995 70553 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194786 70553 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
16117281 60144 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642880 60144 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739648 60144 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16019305 10581 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169898 10581 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799667 10913 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10913 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
16117282 60138 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642888 60138 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739615 60138 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
4106 2502 22 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
5358812 2502 22 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
89 2502 22 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
CHEMBL93240 2502 22 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
20901220 10918 4 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172868 10918 4 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16071727 60102 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642848 60102 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739253 60102 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
10430623 18675 24 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18675 24 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
9950402 170454 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL444878 170454 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435623 148997 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394232 148997 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
49836509 18771 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277999 18771 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
57402070 71563 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71563 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71563 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
18560325 10958 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173284 10958 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
49799664 11001 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173774 11001 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44435612 88796 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236405 88796 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57396850 71524 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71524 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71524 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
24965679 84035 19 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207386 84035 19 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
18590416 10688 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170689 10688 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
57393365 71550 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
53325577 60158 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642874 60158 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739700 60158 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
18560539 10880 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172595 10880 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18560202 10633 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170274 10633 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16117279 60136 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 60136 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 60136 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
11316536 201779 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606765 201779 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44388951 62529 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178234 62529 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
563919 99278 5 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL281937 99278 5 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
20901117 10676 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10676 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019610 10864 10 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172404 10864 10 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
71769424 91955 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414704 91955 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
118727447 117438 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
CHEMBL3398395 117438 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
44435619 88783 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236335 88783 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118512792 145121 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3911908 145121 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
18591074 10894 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172723 10894 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
46224941 199149 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589386 199149 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
18560060 10908 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172790 10908 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7184895 10651 6 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170439 10651 6 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16118795 60096 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 60096 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 60096 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
86302554 110833 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110833 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
45484298 197297 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568673 197297 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45113400 14231 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099284 14231 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199172 14231 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
10291754 70434 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL194590 70434 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
25067564 201300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 201300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
20901261 10678 7 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170679 10678 7 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
20901266 10911 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172793 10911 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
20901268 11002 5 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173777 11002 5 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224944 199577 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL592516 199577 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
16019510 10999 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173706 10999 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
23652787 56688 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642419 56688 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
20901258 10949 3 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173207 10949 3 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
56849580 68875 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922620 68875 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318111 60088 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642862 60088 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739117 60088 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53318268 57661 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668582 57661 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
25117680 200635 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 200635 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
7184976 10735 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171092 10735 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54586812 62717 5 None -12 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783953 62717 5 None -12 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
42631003 199618 13 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 199618 13 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
16718922 198220 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
CHEMBL575310 198220 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
54582940 62722 5 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783958 62722 5 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
16117153 60139 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 60139 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 60139 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
53324896 57664 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668585 57664 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
25123013 200458 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 200458 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44155109 8174 4 None 21 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8174 4 None 21 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46227396 201640 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 201640 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
16019453 10940 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173127 10940 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24894055 183168 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL479548 183168 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
18590411 10923 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172938 10923 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
71813838 91591 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407545 91591 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
46224880 200870 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL601304 200870 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
71695200 129762 6 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129762 6 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44388970 64856 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182099 64856 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880708 7446 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1086719 7446 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
49836823 18710 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
CHEMBL1277466 18710 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
23655467 89390 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
CHEMBL236988 89390 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
25117677 200252 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 200252 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
126720440 163026 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175829 163026 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
24771124 184334 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484333 184334 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019580 10563 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10563 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16019288 10691 7 None 234 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170696 10691 7 None 234 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019550 10707 14 None 131 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170886 10707 14 None 131 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901217 10907 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172789 10907 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
56849581 68876 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68876 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849715 68879 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922624 68879 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16118796 60098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642853 60098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739217 60098 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18559973 10637 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170280 10637 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224918 199493 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591801 199493 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
45483622 198091 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574403 198091 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
52918030 57648 4 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668569 57648 4 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
129103318 167314 0 None -19 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167314 0 None -19 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
118512804 157664 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
CHEMBL4081529 157664 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
23653062 56693 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642424 56693 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
57396848 71536 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71536 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71536 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
46880532 6300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081794 6300 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
16019609 10612 10 None 223 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170098 10612 10 None 223 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224914 199546 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592271 199546 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
71769065 91958 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414711 91958 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
20901172 10583 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169900 10583 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
118727442 117433 0 None -5 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398389 117433 0 None -5 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
56849581 68876 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68876 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44435615 89141 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236578 89141 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
53319627 57660 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668581 57660 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
53323599 57654 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668575 57654 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
53320009 56663 0 None 2 7 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56663 0 None 2 7 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
53323402 60142 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642864 60142 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739646 60142 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117283 60148 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1642883 60148 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1739658 60148 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
3232 3509 19 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
3248571 3509 19 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
CHEMBL60264 3509 19 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
53326177 57667 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57667 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
44388931 64114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180826 64114 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
7185122 10608 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170093 10608 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901254 10910 8 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172792 10910 8 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
7470702 10652 10 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170442 10652 10 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
16019490 11000 5 None 8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173709 11000 5 None 8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
18590413 10982 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173503 10982 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16222547 82038 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165541 82038 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
45487150 197720 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL571413 197720 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
56849714 68878 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922623 68878 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46224945 201406 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL604669 201406 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49799663 10674 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170664 10674 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
20901114 10941 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173132 10941 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
131999484 182603 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182603 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182603 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
49836924 18773 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
CHEMBL1278000 18773 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
44156626 57669 4 None - 1 Human 8.7 pIC50 = 8.7 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668590 57669 4 None - 1 Human 8.7 pIC50 = 8.7 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44554228 18742 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277752 18742 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44389016 63920 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180606 63920 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
11256720 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
9444 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
CHEMBL1083390 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
DB12680 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
11256720 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
11256720 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
9444 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL1083390 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
DB12680 2055 79 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
49836824 18711 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277467 18711 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44554227 18750 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18750 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
135398737 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
38 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
722 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
CHEMBL42 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
DB00363 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
135398737 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
38 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
722 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
CHEMBL42 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
DB00363 958 93 None -7 43 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
7185123 10677 6 None 851 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10677 6 None 851 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901267 10947 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1173205 10947 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
16019602 10687 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170688 10687 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
25117681 200556 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599023 200556 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
20901132 10843 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172207 10843 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18560542 10906 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1172788 10906 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
71770944 91965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
CHEMBL2414732 91965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
71770944 91965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
CHEMBL2414732 91965 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
16222549 82020 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165524 82020 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
54583938 62733 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783970 62733 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
46225002 199494 5 None -602 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591803 199494 5 None -602 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
16116900 60101 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642847 60101 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739252 60101 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
57398718 69745 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69745 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
118173755 192334 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206617 192334 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
10141477 140258 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380556 140258 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
11177383 201732 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606549 201732 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
46227404 199883 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL594548 199883 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11235953 201786 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606815 201786 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
118727445 117436 0 None -8 3 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398392 117436 0 None -8 3 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
44435617 89142 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236579 89142 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
20901163 10976 8 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173434 10976 8 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
58357790 129766 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3675195 129766 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
16019312 10898 1 None 144 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172727 10898 1 None 144 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
58357705 129030 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
CHEMBL3670284 129030 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
20901131 10568 7 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1169725 10568 7 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
49799645 10895 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172724 10895 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
57403833 71470 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71470 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71470 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44126328 201105 5 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL603049 201105 5 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
68303508 129763 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675192 129763 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53323439 60157 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642873 60157 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739699 60157 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44435621 88784 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236336 88784 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24965329 84037 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207388 84037 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
46225027 199117 5 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589150 199117 5 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44474625 14071 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197521 14071 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL575270 14071 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
20901145 10810 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171992 10810 1 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322935 57668 4 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668589 57668 4 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44403103 141309 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL383373 141309 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44263496 201525 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL605292 201525 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
71770821 91962 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414725 91962 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
118512815 151677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3964100 151677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
118727448 117439 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
CHEMBL3398396 117439 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
57403837 71473 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71473 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71473 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
24783810 176197 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459371 176197 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
10274389 133422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370507 133422 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46189987 68889 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1922634 68889 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11775364 201787 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 201787 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
20901128 10950 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173208 10950 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18591272 10660 9 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170473 10660 9 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
16750338 62629 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783607 62629 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
118727450 117441 0 None -5 3 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398398 117441 0 None -5 3 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
46224878 199469 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591568 199469 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
44433194 146602 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392318 146602 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11545169 147651 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393158 147651 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263299 192118 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520343 192118 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
21071390 1987 53 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
8689 1987 53 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
CHEMBL3286580 1987 53 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
DB11957 1987 53 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
46190034 68891 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922636 68891 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
25122652 200662 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 200662 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
25263301 184619 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484927 184619 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019601 10564 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169708 10564 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901120 10634 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170275 10634 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799683 10942 3 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173135 10942 3 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
45113275 9107 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099282 9107 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
16117280 60137 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642887 60137 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739614 60137 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
57393363 71564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71564 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
44156863 8078 0 None 21 2 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 8078 0 None 21 2 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
16019372 10680 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170681 10680 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
44126269 201484 5 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 201484 5 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44435631 89677 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237594 89677 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122651 200249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 200249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
18560562 10613 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170099 10613 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
45113535 14240 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1097614 14240 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1199305 14240 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
57403835 71471 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949767 71471 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962397 71471 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
46224915 199575 3 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592514 199575 3 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
18591268 10899 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172728 10899 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118173772 190375 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5177311 190375 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
20901118 10562 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169706 10562 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
18560182 10863 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172403 10863 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
71769190 91960 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414713 91960 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
23624297 56682 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642413 56682 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
45487139 197340 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL568935 197340 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
46224942 201405 3 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL604668 201405 3 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
118727449 117440 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398397 117440 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54579956 62720 5 None -3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783956 62720 5 None -3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
53326176 57665 4 None - 1 Human 8.5 pIC50 = 8.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57665 4 None - 1 Human 8.5 pIC50 = 8.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
10405986 18789 1 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1278092 18789 1 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
57396970 69743 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69743 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
118181460 189893 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5169546 189893 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44327759 207912 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL96745 207912 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
16071847 60145 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 60145 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 60145 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44389002 63564 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180066 63564 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
53318109 60103 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642849 60103 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739254 60103 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
18560186 10582 10 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169899 10582 10 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10356663 111943 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111943 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
58357851 129026 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670280 129026 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357730 129032 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
CHEMBL3670286 129032 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
57398615 71549 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71549 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71549 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44389074 123312 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361572 123312 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
71814157 91595 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407553 91595 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
71814318 91596 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
CHEMBL2407554 91596 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
23653135 56681 3 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642412 56681 3 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
25117679 200604 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 200604 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
57400392 69753 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69753 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
18560181 10711 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170892 10711 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
44155109 8174 4 None 21 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8174 4 None 21 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
10356663 111943 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL328816 111943 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
53322548 56687 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642418 56687 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
54580942 62731 9 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783967 62731 9 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
71813833 91589 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407540 91589 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
57391618 71469 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71469 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71469 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
25122654 200528 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 200528 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
44388944 63018 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178767 63018 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
118512805 147564 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3930881 147564 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836715 18662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277010 18662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
44435633 89541 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237389 89541 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57391729 69746 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69746 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
16019553 10706 6 None 912 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10706 6 None 912 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44435609 154402 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398808 154402 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45113404 14222 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095273 14222 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199078 14222 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
58357665 129037 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670292 129037 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
164622805 185863 0 None -30 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185863 0 None -30 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
44155107 8079 4 None 60 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 8079 4 None 60 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16019339 10604 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170087 10604 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
16019508 10912 9 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172794 10912 9 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
57395082 71544 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949766 71544 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963006 71544 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57520121 73267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
CHEMBL2012637 73267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
57520121 73267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
CHEMBL2012637 73267 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
73347610 91956 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414705 91956 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
60141574 73268 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012639 73268 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
18560538 10603 9 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170086 10603 9 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
621659 62729 10 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783965 62729 10 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
7184886 10606 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10606 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224973 199617 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL592751 199617 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49836620 18654 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276925 18654 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
45378935 199505 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591939 199505 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
73349123 91957 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414707 91957 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
18590836 10566 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169722 10566 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
45487129 197806 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL572092 197806 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
25117676 200459 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 200459 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
135339817 181484 0 None -6 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 181484 0 None -6 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
45113401 9109 1 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
CHEMBL1099285 9109 1 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
118727451 117442 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
CHEMBL3398399 117442 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
10286610 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL355905 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52918032 57643 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668564 57643 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
53322258 57644 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668565 57644 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357784 129035 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670290 129035 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
53326178 57675 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668596 57675 4 None - 1 Human 8.4 pIC50 = 8.4 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
44389023 62515 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
CHEMBL178193 62515 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
44554393 18547 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18547 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
4106 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
4106 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2502 22 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
57400234 71540 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71540 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71540 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
49836716 18663 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1277011 18663 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
7184883 10896 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10896 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
118512841 156456 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
CHEMBL4067243 156456 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
44126327 201653 5 None -41 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL606036 201653 5 None -41 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
45487128 197787 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571878 197787 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
18560556 10917 11 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172867 10917 11 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
53320926 57646 4 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1668567 57646 4 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
9929294 64080 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180765 64080 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44388999 63381 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179592 63381 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
10115854 69599 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193450 69599 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
54581998 62735 3 None -5 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783972 62735 3 None -5 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
45378936 199506 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 199506 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
54581997 62730 6 None -11 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783966 62730 6 None -11 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
16117152 60086 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642885 60086 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739101 60086 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
44126330 62724 5 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783960 62724 5 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
57520122 73269 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012643 73269 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
45378934 201646 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 201646 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
57396813 71545 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
53323601 57672 4 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57672 4 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
46189980 68894 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68894 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
21254909 57621 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668501 57621 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318142 60090 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642867 60090 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739135 60090 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16049388 82023 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165527 82023 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
20901141 10708 6 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170887 10708 6 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
10068007 18787 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278090 18787 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
44474631 14082 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197618 14082 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL578631 14082 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
7246142 10922 8 None 85 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172934 10922 8 None 85 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901139 10956 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173282 10956 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53320927 57649 4 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668570 57649 4 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
71770822 91963 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
CHEMBL2414726 91963 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
46884709 8080 4 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 8080 4 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16116898 60128 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1642877 60128 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1739545 60128 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
18591271 10657 12 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170466 10657 12 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901160 10916 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172866 10916 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
44403097 72446 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198827 72446 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44435644 89129 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236571 89129 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118727443 117434 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398390 117434 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
44516817 57663 5 None 1023 2 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668584 57663 5 None 1023 2 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44156624 57670 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668591 57670 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
162646407 179623 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4742804 179623 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
45484340 196826 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565746 196826 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
162656068 180816 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756814 180816 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
44435603 91750 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL240922 91750 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435640 154929 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL401019 154929 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
49799684 10943 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173136 10943 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901125 10977 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173435 10977 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
6625986 10605 10 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170088 10605 10 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
25123012 201709 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
CHEMBL606401 201709 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
126720394 162314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164541 162314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357663 129029 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670283 129029 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357754 129033 4 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670288 129033 4 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
9924959 69464 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193358 69464 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
16019364 10957 6 None 53 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173283 10957 6 None 53 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
53318300 57619 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668499 57619 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
71813685 91597 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407562 91597 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
18559939 10632 12 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170273 10632 12 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24794436 14069 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL1197511 14069 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL574856 14069 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
25263300 184618 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484926 184618 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
10136837 165963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
CHEMBL425196 165963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
10136837 165963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL425196 165963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44474797 14064 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL1197505 14064 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574625 14064 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
49836508 18770 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
CHEMBL1277998 18770 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
57402187 69750 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69750 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
20901263 10679 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170680 10679 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956087 10981 10 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1173502 10981 10 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
49836619 18644 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276839 18644 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
46224916 199470 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL591569 199470 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
46224943 199576 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592515 199576 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
53319441 60099 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642845 60099 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739231 60099 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
44435622 89100 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236540 89100 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403099 133010 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370215 133010 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
126720425 162114 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161308 162114 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357826 129767 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL3675196 129767 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
118512827 146431 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3921947 146431 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836618 18643 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276838 18643 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
18560564 10614 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170100 10614 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224877 200701 5 None -74 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL599913 200701 5 None -74 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
23725134 14054 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL1197475 14054 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL573521 14054 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
71813986 91592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407547 91592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
20901126 10565 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169709 10565 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956089 10893 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172722 10893 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
7184892 10937 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173063 10937 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799656 10974 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10974 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10974 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54584885 62726 5 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783962 62726 5 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44474470 14061 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL1197489 14061 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL573981 14061 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
16019546 10710 6 None 676 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170891 10710 6 None 676 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901133 10636 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170279 10636 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901186 10638 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170281 10638 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019514 10866 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172406 10866 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44224259 62723 5 None -30 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783959 62723 5 None -30 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44155109 8174 4 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1091919 8174 4 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
57400234 71540 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71540 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71540 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
44156863 8078 0 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 8078 0 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
44156622 57671 4 None - 1 Human 8.2 pIC50 = 8.2 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668592 57671 4 None - 1 Human 8.2 pIC50 = 8.2 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
10449488 196866 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565976 196866 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
118181414 191195 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5189271 191195 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
126720397 181095 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760105 181095 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
162644347 181759 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4777550 181759 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
57393468 69752 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69752 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
46880757 6028 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080381 6028 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
20901264 10965 8 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173360 10965 8 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901122 10586 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169903 10586 6 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
18560317 10915 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172862 10915 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
68261572 129764 5 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675193 129764 5 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
10140915 140355 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380772 140355 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
20901229 10983 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173506 10983 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
11595209 94841 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253708 94841 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
49836616 18803 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278179 18803 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
45113534 14228 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1097613 14228 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199141 14228 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
45113399 9108 4 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
CHEMBL1099283 9108 4 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
57391567 71537 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71537 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71537 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
20901115 10964 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10964 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118727444 117435 0 None -25 2 Human 5.2 pIC50 = 5.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398391 117435 0 None -25 2 Human 5.2 pIC50 = 5.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54585847 62732 6 None -29 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783968 62732 6 None -29 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
44435626 154858 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
CHEMBL400608 154858 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
16019397 10959 11 None 54 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173286 10959 11 None 54 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
71769315 91961 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414722 91961 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
44126325 199114 5 None -10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589147 199114 5 None -10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
57396813 71545 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
20901210 10919 4 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172869 10919 4 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
71813835 91590 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
CHEMBL2407542 91590 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
20901259 10966 6 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173361 10966 6 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57393467 69748 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935595 69748 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
18560324 10709 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170890 10709 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
44435630 89676 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL237593 89676 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
7185121 10607 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170092 10607 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901265 10734 7 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1171041 10734 7 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
126720403 162610 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162610 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
16019574 10881 11 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172596 10881 11 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901253 10921 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172933 10921 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46225000 199115 5 None -9 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589148 199115 5 None -9 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
118181454 189961 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5170650 189961 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
9969402 70547 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194750 70547 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44403104 72479 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198941 72479 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44155107 8079 4 None 60 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 8079 4 None 60 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
44537940 18774 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18774 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
44403065 166312 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL427184 166312 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46830134 8217 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8217 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46830134 8217 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8217 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44435632 89469 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237179 89469 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122653 200527 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 200527 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
71813988 91593 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407549 91593 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
16019519 10968 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173364 10968 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
58357699 129034 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670289 129034 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
53316984 57647 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668568 57647 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16019303 10600 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170069 10600 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901275 10661 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170474 10661 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019310 10759 11 None 47 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1171436 10759 11 None 47 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
71815503 117437 0 None -3 3 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398394 117437 0 None -3 3 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
71769066 91959 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414712 91959 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
54585848 62734 6 None -5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783971 62734 6 None -5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901142 10763 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1171500 10763 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
24763352 62623 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783601 62623 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
46880759 6132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080899 6132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
53319628 57662 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668583 57662 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
44403089 133629 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL371469 133629 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
24783294 176712 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
CHEMBL459987 176712 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
71814155 91594 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407551 91594 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
20901136 10969 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173365 10969 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
45113530 14223 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095274 14223 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199079 14223 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
46189982 129765 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675194 129765 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
18591267 10639 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170282 10639 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799656 10974 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10974 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10974 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57391567 71537 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71537 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71537 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
18560184 10862 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172398 10862 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
86302554 110833 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110833 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
44433199 88776 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236314 88776 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24771120 184100 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 184100 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
9978683 18674 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18674 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
16118923 60146 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 60146 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 60146 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
44403093 71438 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196094 71438 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
9950255 196815 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565723 196815 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
57398803 69742 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69742 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69742 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
44388956 63087 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178870 63087 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
10383646 18762 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18762 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
44389003 123836 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362487 123836 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880709 7447 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
CHEMBL1086720 7447 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
20901169 10686 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170687 10686 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
11723168 207494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL94422 207494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
44397689 71440 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196102 71440 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL373107 71440 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
46880758 6095 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080729 6095 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
16019343 10580 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1169894 10580 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
20901124 10631 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170271 10631 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
18591266 10927 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173004 10927 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
45487140 198833 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583677 198833 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
54582938 62719 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783955 62719 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
58357860 129027 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670281 129027 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
45113403 9068 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1098894 9068 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
9842551 127223 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365774 127223 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44126329 62718 6 None 2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783954 62718 6 None 2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18560255 10715 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170897 10715 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18559286 10990 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173575 10990 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7183407 10991 12 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173576 10991 12 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
162647425 179577 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4741978 179577 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
16116896 60140 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642861 60140 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739644 60140 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
53320746 60150 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642854 60150 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739685 60150 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
46224879 201547 3 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 201547 3 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
49799629 10936 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173062 10936 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512807 150392 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3953555 150392 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
16116899 60100 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642846 60100 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739232 60100 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
25123011 201193 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 201193 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
11723168 207494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL94422 207494 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
197033 199152 64 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL589390 199152 64 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18559285 10924 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172939 10924 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
197033 199152 64 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 199152 64 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
54579957 62728 5 None -36 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783964 62728 5 None -36 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
56849578 68873 4 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922618 68873 4 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189935 68888 3 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68888 3 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44389099 64837 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182000 64837 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44389015 122330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359876 122330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435538 90606 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
CHEMBL238770 90606 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
44388943 63290 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL179277 63290 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
53327611 69754 0 None 154 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None 154 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
53323436 60132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642870 60132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739585 60132 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16019366 10675 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170671 10675 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
18559353 10640 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170288 10640 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
53326022 60141 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642863 60141 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739645 60141 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44435618 88782 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236334 88782 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46224881 200963 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL601902 200963 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
53323600 57658 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668579 57658 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
20901270 10656 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170465 10656 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
16019292 10993 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10993 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53319443 60154 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642858 60154 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739696 60154 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
16956204 10980 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173501 10980 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117154 60147 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642881 60147 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739657 60147 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
46880658 6380 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1082199 6380 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
16118797 60097 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642852 60097 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739216 60097 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
44435620 148994 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394231 148994 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44474629 14079 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL1197581 14079 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL577570 14079 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
57393365 71550 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
23624309 176733 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460195 176733 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
44403092 70634 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL195018 70634 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10272325 71741 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL196619 71741 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
16019394 10865 8 None 37 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172405 10865 8 None 37 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019604 10973 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173431 10973 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
3241 3521 24 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918649 3521 24 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
CHEMBL1210710 3521 24 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
11256720 2055 79 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
9444 2055 79 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
CHEMBL1083390 2055 79 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
DB12680 2055 79 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
44126272 199150 5 None -14 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589388 199150 5 None -14 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
44126326 199619 7 None -32 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592753 199619 7 None -32 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
46884709 8080 4 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091208 8080 4 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
58357740 129031 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3670285 129031 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
58158749 138995 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785512 138995 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
54752954 138950 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785100 138950 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
46189932 68885 4 None - 1 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68885 4 None - 1 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56655504 68869 3 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68869 3 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44216882 139115 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786752 139115 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
58158721 138992 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785453 138992 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595671 65678 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834333 65678 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
6918542 204924 24 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 204924 24 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44240860 139182 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787525 139182 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593934 65695 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65695 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
56595402 65637 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595531 65646 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
CHEMBL1834235 65646 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
56593797 65687 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834341 65687 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
56593933 65694 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
CHEMBL1834349 65694 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
58158719 138991 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785431 138991 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
59339383 139136 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787014 139136 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595670 65677 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834332 65677 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
56593643 65680 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834335 65680 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56593803 65691 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
CHEMBL1834346 65691 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
58158748 139093 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786563 139093 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
10356663 111943 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111943 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
56595667 65651 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834241 65651 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158707 139048 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786087 139048 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595533 65647 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
CHEMBL1834237 65647 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
56593799 65689 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834343 65689 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127033666 138971 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785278 138971 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595280 65636 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834225 65636 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
25056080 65690 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65690 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
56595280 65636 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834225 65636 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
25056080 65690 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834345 65690 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593644 65681 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834336 65681 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127031618 139169 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
CHEMBL3787388 139169 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
56595529 65645 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
CHEMBL1834234 65645 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
56595529 65645 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
CHEMBL1834234 65645 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
56593646 65683 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834338 65683 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
58158738 138962 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785231 138962 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593642 65679 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834334 65679 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158668 139028 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785864 139028 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593798 65688 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834342 65688 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
58158739 139157 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787201 139157 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56593932 65693 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
CHEMBL1834348 65693 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
59339335 139006 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785626 139006 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
53310757 139134 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786973 139134 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56849719 68882 3 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68882 3 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56595402 65637 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595668 65652 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834242 65652 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595405 65640 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
70878688 65640 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
CHEMBL1834229 65640 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
56595535 65649 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
CHEMBL1834239 65649 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
56595402 65637 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595402 65637 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834226 65637 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
44240753 139110 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786693 139110 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
44240802 139181 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787508 139181 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595403 65638 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834227 65638 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
24855787 65634 1 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834221 65634 1 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56595404 65639 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
CHEMBL1834228 65639 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
56595666 65650 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834240 65650 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
56593931 65692 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
CHEMBL1834347 65692 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
56593936 65697 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834352 65697 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
56593936 65697 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834352 65697 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
127032424 139111 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786703 139111 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595406 65642 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
CHEMBL1834230 65642 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
56595534 65648 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
CHEMBL1834238 65648 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
56593645 65682 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834337 65682 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
56593647 65684 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834339 65684 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
56665086 65686 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834340 65686 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
58158682 138967 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785259 138967 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595407 65643 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
CHEMBL1834231 65643 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
56595669 65653 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834243 65653 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158709 139159 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787246 139159 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595408 65644 0 None - 0 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
CHEMBL1834232 65644 0 None - 0 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
56849576 68871 4 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68871 4 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849576 68871 4 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68871 4 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
10131620 102478 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413990 102478 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040186 102478 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44156626 57669 4 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668590 57669 4 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
56655571 68887 36 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922632 68887 36 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849575 68870 4 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922615 68870 4 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326176 57665 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668586 57665 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44516817 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668584 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156754 6510 4 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6510 4 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
44516817 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44516817 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44516817 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57663 5 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918032 57643 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668564 57643 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
53322258 57644 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668565 57644 4 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56655504 68869 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68869 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 19 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 19 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 19 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
56849579 68874 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922619 68874 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44156628 6714 4 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6714 4 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44156622 57671 4 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668592 57671 4 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
44156752 6580 4 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6580 4 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
46190037 68893 2 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922638 68893 2 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326177 57667 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668588 57667 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156624 57670 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668591 57670 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
46189932 68885 4 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68885 4 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46867519 6508 4 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6508 4 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
46189984 68890 1 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922635 68890 1 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53316984 57647 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668568 57647 4 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849578 68873 4 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922618 68873 4 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53326178 57675 4 None - 1 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668596 57675 4 None - 1 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
46189935 68888 3 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922633 68888 3 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46190034 68891 0 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922636 68891 0 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 19 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 19 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 19 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
44155994 57650 4 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668571 57650 4 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
6918479 56661 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
CHEMBL1642114 56661 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
56849857 68892 3 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922637 68892 3 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
56655505 68884 3 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922629 68884 3 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44155992 57651 4 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668572 57651 4 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
53322935 57668 4 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668589 57668 4 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
44155874 57620 22 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668500 57620 22 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44155874 57620 22 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668500 57620 22 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579181 190952 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
CHEMBL518591 190952 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
46890885 6901 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1084315 6901 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46189980 68894 3 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922639 68894 3 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
6918629 68918 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922716 68918 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
46189987 68889 3 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922634 68889 3 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
53324896 57664 4 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668585 57664 4 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110702 171277 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL446054 171277 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579085 190440 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517828 190440 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9944808 102470 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413989 102470 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040139 102470 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476436 82347 6 None 7413 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 82347 6 None 7413 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
56849717 68881 3 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922626 68881 3 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849716 68880 2 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922625 68880 2 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476434 82346 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172185 82346 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
44155875 60983 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1762568 60983 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
10286330 182800 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
CHEMBL479067 182800 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
44579131 181624 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
CHEMBL477386 181624 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
44579182 182641 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478871 182641 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53320929 57673 4 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668594 57673 4 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
5113605 79723 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL211577 79723 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
44579132 181625 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477387 181625 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46891114 6625 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1083298 6625 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
46891174 6884 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1084214 6884 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
53323601 57672 4 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668593 57672 4 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
56849713 68877 3 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68877 3 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849713 68877 3 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68877 3 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3509 19 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 19 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 19 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
53318300 57619 0 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668499 57619 0 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44476804 82350 2 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172190 82350 2 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
9822810 69502 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69502 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
46882521 5711 0 None - 2 Human 6.9 pKi = 6.9 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5711 0 None - 2 Human 6.9 pKi = 6.9 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
46891053 6511 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082764 6511 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891175 6943 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084482 6943 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
53323599 57654 4 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668575 57654 4 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
52915983 60989 5 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762574 60989 5 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
44476607 82352 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172192 82352 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
44156502 60984 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762569 60984 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
58149665 82344 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172183 82344 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
45488151 196910 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
CHEMBL566213 196910 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
53320927 57649 4 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668570 57649 4 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
46882583 5756 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
CHEMBL1078491 5756 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
68014793 91928 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413987 91928 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
53324895 57645 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
CHEMBL1668566 57645 4 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
45102707 5757 0 None - 1 Human 6.8 pKi = 6.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
CHEMBL1078492 5757 0 None - 1 Human 6.8 pKi = 6.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
46890103 7149 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085361 7149 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
31386 96606 95 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL263327 96606 95 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
45488139 196947 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
CHEMBL566410 196947 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
45488143 197766 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
CHEMBL571762 197766 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
21254909 57621 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668501 57621 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849714 68878 3 None - 1 Human 7.8 pKi = 7.8 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922623 68878 3 None - 1 Human 7.8 pKi = 7.8 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488166 196912 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
CHEMBL566219 196912 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
46867655 6656 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
CHEMBL1083389 6656 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
56849577 68872 4 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922617 68872 4 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
10934 1320 115 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
2955 1320 115 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
782 1320 115 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
CHEMBL1043 1320 115 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
DB00250 1320 115 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
46890886 6902 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084316 6902 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46891112 7270 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085965 7270 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46882522 5712 0 None - 2 Human 6.7 pKi = 6.7 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5712 0 None - 2 Human 6.7 pKi = 6.7 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46190041 68895 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922640 68895 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476611 82351 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172191 82351 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
52918030 57648 4 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668569 57648 4 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110703 189720 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL515624 189720 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9924293 68896 0 None - 1 Human 8.6 pKi = 8.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922641 68896 0 None - 1 Human 8.6 pKi = 8.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
54238415 91924 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413983 91924 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
56849581 68876 1 None - 1 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922621 68876 1 None - 1 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53324933 57622 2 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668502 57622 2 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
52915982 60990 3 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762575 60990 3 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
10658135 91926 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413985 91926 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46891113 6624 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083297 6624 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891111 6803 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083909 6803 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891004 7145 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085351 7145 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890058 7249 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085835 7249 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46867524 6583 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083078 6583 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
52915869 60991 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762576 60991 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
45488165 196911 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL566218 196911 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46867523 6582 4 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083077 6582 4 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44155871 60986 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762571 60986 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
52915984 60992 4 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762577 60992 4 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
56849719 68882 3 None - 0 Human 8.5 pKi = 8.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68882 3 None - 0 Human 8.5 pKi = 8.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53322259 57652 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668573 57652 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
53320926 57646 4 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
CHEMBL1668567 57646 4 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
53326175 57659 4 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668580 57659 4 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
53319628 57662 0 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668583 57662 0 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579180 182640 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478870 182640 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53325519 57655 4 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668576 57655 4 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
10132329 102476 1 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413988 102476 1 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040182 102476 1 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
45488131 198581 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
CHEMBL578411 198581 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
46890949 6447 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082485 6447 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890056 6452 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082494 6452 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890946 6598 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1083122 6598 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46891176 6944 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084483 6944 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891005 7146 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085352 7146 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891055 6513 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082766 6513 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891056 6514 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082767 6514 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891007 7148 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
CHEMBL1085354 7148 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
56849720 68883 3 None - 0 Human 7.5 pKi = 7.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922628 68883 3 None - 0 Human 7.5 pKi = 7.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488152 198929 0 None - 0 Mouse 7.5 pKi = 7.5 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 198929 0 None - 0 Mouse 7.5 pKi = 7.5 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
53318267 57656 1 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668577 57656 1 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
53320928 57657 4 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668578 57657 4 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
44579183 182643 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478872 182643 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
56849715 68879 3 None - 1 Human 8.4 pKi = 8.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922624 68879 3 None - 1 Human 8.4 pKi = 8.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849856 68886 5 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922631 68886 5 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53323600 57658 2 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668579 57658 2 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
68014784 91927 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413986 91927 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52915980 60987 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762572 60987 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
77956 73019 88 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2009408 73019 88 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476801 82349 3 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172189 82349 3 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
45488152 198929 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 198929 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
45488152 198929 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 198929 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46890948 6446 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082484 6446 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891006 7147 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085353 7147 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890059 7250 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085836 7250 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
3232 3509 19 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3509 19 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3509 19 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
1472656 34628 25 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1429795 34628 25 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
460659 51406 8 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL1581846 51406 8 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
46882520 5856 0 None - 2 Human 8.2 pKi = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5856 0 None - 2 Human 8.2 pKi = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
44155876 57653 3 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668574 57653 3 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
46891054 6512 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082765 6512 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
46890106 6979 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
CHEMBL1084614 6979 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
45102708 5770 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078595 5770 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
56849580 68875 5 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922620 68875 5 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918031 57666 4 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668587 57666 4 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579130 181623 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477385 181623 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579129 182137 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478223 182137 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579133 190238 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517503 190238 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46890057 6527 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082818 6527 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890105 7197 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085608 7197 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
53319627 57660 1 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668581 57660 1 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
9822810 69502 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69502 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
52915979 60988 5 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762573 60988 5 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
46890947 6445 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082483 6445 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890887 6903 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084317 6903 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46890104 7150 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085362 7150 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
9925009 102477 2 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413991 102477 2 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040183 102477 2 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
640912 91925 7 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413984 91925 7 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46867654 6655 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083388 6655 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
52915868 60985 6 None - 1 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762570 60985 6 None - 1 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
53319629 57674 4 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668595 57674 4 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
4223 3992 94 None -562 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 94 None -562 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 94 None -562 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 94 None -562 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 94 None -562 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
10131112 1552 25 None 14 7 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
8428 1552 25 None 14 7 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
CHEMBL364005 1552 25 None 14 7 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331




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ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

2585 803 103 None -109 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 103 None -109 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 103 None -109 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 103 None -109 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 103 None -109 21 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2726 919 68 None -10 72 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 68 None -10 72 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 68 None -10 72 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 68 None -10 72 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 68 None -10 72 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
135398745 2914 112 None -4 65 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 112 None -4 65 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 112 None -4 65 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 112 None -4 65 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
1209 1658 75 None -12 32 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 75 None -12 32 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 75 None -12 32 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 75 None -12 32 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 75 None -12 32 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
135398737 958 93 None -4 89 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 93 None -4 89 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 93 None -4 89 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 93 None -4 89 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 93 None -4 89 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135409453 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2162 41514 100 None -2 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41514 100 None -2 6 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3158 56267 27 None -851 20 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56267 27 None -851 20 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1400 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 70 None - 3 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
191 403 98 None -20 29 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 98 None -20 29 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 98 None -20 29 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 98 None -20 29 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 98 None -20 29 Human 7.6 pAC50 = 7.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
5329102 194726 86 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194726 86 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
2284 3182 33 None -12 29 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 33 None -12 29 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 33 None -12 29 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 33 None -12 29 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 33 None -12 29 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
6918638 157987 97 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 5 3 4 2.0 O=C(/C=C/c1cccc(S(=O)(=O)Nc2ccccc2)c1)NO 10.1038/s41467-023-40064-9
CHEMBL408513 157987 97 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 5 3 4 2.0 O=C(/C=C/c1cccc(S(=O)(=O)Nc2ccccc2)c1)NO 10.1038/s41467-023-40064-9
1971 2866 38 None -14 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 38 None -14 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 38 None -14 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 38 None -14 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 38 None -14 30 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
3294 2006 111 None -87 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 111 None -87 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 111 None -87 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 111 None -87 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 111 None -87 45 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2247 505 81 None -53 42 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 81 None -53 42 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 81 None -53 42 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 81 None -53 42 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 81 None -53 42 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
1427 2013 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 54 None - 27 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
21722 17992 31 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17992 31 None - 6 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
212 3806 47 None -6 25 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3806 47 None -6 25 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3806 47 None -6 25 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3806 47 None -6 25 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3806 47 None -6 25 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
1224 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 83 None - 13 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2337 3256 77 None -54 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 77 None -54 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 77 None -54 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 77 None -54 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 77 None -54 62 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
1613 2348 53 None -5 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 53 None -5 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 53 None -5 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 53 None -5 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 53 None -5 44 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2389 3331 118 None -2570 67 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 118 None -2570 67 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 118 None -2570 67 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 118 None -2570 67 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 118 None -2570 67 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
135 2532 43 None -21 58 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 43 None -21 58 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 43 None -21 58 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 43 None -21 58 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 43 None -21 58 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
102 4127 48 None -173 49 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4127 48 None -173 49 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4127 48 None -173 49 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4127 48 None -173 49 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4127 48 None -173 49 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
2600 3779 74 None -5 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 74 None -5 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 74 None -5 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 74 None -5 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 74 None -5 13 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1890 2759 49 None - 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 49 None - 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 49 None - 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 49 None - 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 49 None - 16 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR6 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
9921064 127178 25 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 127178 25 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
10337743 4076 18 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
8429 4076 18 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
CHEMBL571858 4076 18 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
91971999 138831 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781299 138831 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
46189984 68890 1 None - 1 Human 9.6 pIC50 = 9.6 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68890 1 None - 1 Human 9.6 pIC50 = 9.6 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
118465011 138833 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781323 138833 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
56655504 68869 3 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68869 3 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465045 138768 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780579 138768 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
52918031 57666 4 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57666 4 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465023 138839 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781452 138839 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118464996 138717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3779904 138717 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
46189935 68888 3 None - 1 Human 9.3 pIC50 = 9.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68888 3 None - 1 Human 9.3 pIC50 = 9.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189980 68894 3 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68894 3 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189932 68885 4 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68885 4 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465171 138745 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780274 138745 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
10383682 120389 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
CHEMBL353389 120389 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
53326176 57665 4 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57665 4 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
44476436 82347 6 None - 1 Human 9.1 pIC50 = 9.1 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172186 82347 6 None - 1 Human 9.1 pIC50 = 9.1 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
53326177 57667 4 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57667 4 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
118464995 138818 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781179 138818 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
44155109 8174 4 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8174 4 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44156863 8078 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 8078 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
118464998 138867 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781801 138867 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
118465054 138828 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781263 138828 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
44155107 8079 4 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 8079 4 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
118465064 138723 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779974 138723 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
68303363 129760 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
CHEMBL3675189 129760 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
118465035 138731 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780141 138731 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118464997 138824 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781239 138824 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
10427672 104994 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113554 104994 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
118465048 138725 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3780011 138725 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
70245924 82353 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172193 82353 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
46830134 8217 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8217 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44476514 82348 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172187 82348 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
118465025 138837 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781399 138837 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
196129 67798 17 None 1 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67798 17 None 1 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
118465050 138795 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780861 138795 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
15619875 69460 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL193351 69460 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
73354882 89693 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89693 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89698 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89698 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 72 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 72 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 72 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 72 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
44403367 71075 4 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL195239 71075 4 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
73351904 89700 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376489 89700 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73353367 89704 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
CHEMBL2376493 89704 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
73351905 89702 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376491 89702 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
4189 206922 96 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 96 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 96 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
3198 205513 76 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 76 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 76 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
135398737 958 93 None -4 89 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None -4 89 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None -4 89 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None -4 89 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None -4 89 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
118465024 138827 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781260 138827 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118465038 138873 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781948 138873 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
53322638 56675 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642128 56675 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
10451504 104957 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
CHEMBL3113350 104957 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
20901117 10676 3 None - 1 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10676 3 None - 1 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
6761 67799 19 None -9 18 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 19 None -9 18 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44155876 57653 3 None - 1 Human 7.0 pIC50 = 7.0 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668574 57653 3 None - 1 Human 7.0 pIC50 = 7.0 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
4601 206747 35 None -2 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 35 None -2 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 35 None -2 16 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
1530 2182 50 None -58 21 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -58 21 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -58 21 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -58 21 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -58 21 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
49864601 15663 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222137 15663 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
1588 2325 27 None -21 44 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 27 None -21 44 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 27 None -21 44 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 27 None -21 44 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 27 None -21 44 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
11724112 104967 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113360 104967 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
9979748 105001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113561 105001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
10472756 104962 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
CHEMBL3113355 104962 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
5 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
2812 4779 101 None -36 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -36 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
11743064 35953 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL144265 35953 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
448537 160250 89 None -35 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160250 89 None -35 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
53319229 56571 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
CHEMBL1641610 56571 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
44476704 82343 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172182 82343 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
135398745 2914 112 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 112 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 112 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 112 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
18180076 15602 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221497 15602 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
5 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 72 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
2600 3779 74 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3779 74 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3779 74 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3779 74 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3779 74 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5323 202789 103 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
CHEMBL62193 202789 103 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
11236269 129305 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
CHEMBL367088 129305 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
11113605 10507 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10507 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
54576142 66495 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852341 66495 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216098 66495 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
180 401 56 None -99 40 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -99 40 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -99 40 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -99 40 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -99 40 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
156018181 177807 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
CHEMBL4643549 177807 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
4211 57822 83 None 1 4 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57822 83 None 1 4 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
45109862 7434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 7434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
52915868 60985 6 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762570 60985 6 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
73453 29616 24 None -10 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29616 24 None -10 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
53318694 56674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642127 56674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
68262106 129761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675190 129761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
2585 803 103 None -109 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 103 None -109 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 103 None -109 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 103 None -109 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 103 None -109 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1548953 207679 27 None -3 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207679 27 None -3 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
11071079 110593 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110593 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
134551 358 27 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 358 27 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 358 27 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 358 27 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
118465034 138744 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780270 138744 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
46866711 15670 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
CHEMBL1222234 15670 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
169713 80161 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 80161 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
6918647 100746 2 None 50 14 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
CHEMBL292759 100746 2 None 50 14 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
58149663 127422 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659969 127422 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
3117 207841 103 None -5 16 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -5 16 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
134 2514 24 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2514 24 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2514 24 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2514 24 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2514 24 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
53321318 56668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642121 56668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
1209 1658 75 None -12 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1658 75 None -12 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1658 75 None -12 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1658 75 None -12 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1658 75 None -12 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
124 2981 47 None -100 33 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 47 None -100 33 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 47 None -100 33 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 47 None -100 33 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 47 None -100 33 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
54577891 66575 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 66575 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 66575 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
102 4127 48 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4127 48 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4127 48 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4127 48 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4127 48 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
53323972 56667 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642120 56667 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
135398737 958 93 None -4 89 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
38 958 93 None -4 89 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
722 958 93 None -4 89 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
CHEMBL42 958 93 None -4 89 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
DB00363 958 93 None -4 89 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
46884709 8080 4 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 8080 4 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
20901115 10964 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10964 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
126720440 163026 0 None 72 5 Human 7.8 pIC50 = 7.8 Binding
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4175829 163026 0 None 72 5 Human 7.8 pIC50 = 7.8 Binding
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
71695200 129762 6 None - 0 Human 6.8 pIC50 = 6.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129762 6 None - 0 Human 6.8 pIC50 = 6.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
3397 205488 112 None - 1 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 205488 112 None - 1 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
53323601 57672 4 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57672 4 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
11741686 104958 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
CHEMBL3113351 104958 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
5 139 72 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 72 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 72 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 72 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
25070582 61454 28 None - 1 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61454 28 None - 1 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
6075 150108 42 None -13 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 42 None -13 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
2291 3184 58 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3184 58 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3184 58 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3184 58 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3184 58 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
7185124 10953 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173210 10953 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
45278882 7452 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 7452 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
176 398 66 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
42635204 187759 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495678 187759 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
10826203 161845 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
CHEMBL414668 161845 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
118465009 138877 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3782008 138877 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
73356447 89706 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
CHEMBL2376561 89706 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
11724023 104969 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113362 104969 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
276 3513 50 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
5312149 3513 50 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
CHEMBL431298 3513 50 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
1043 1582 14 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1582 14 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1582 14 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1582 14 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1582 14 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
118465087 138720 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779933 138720 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118465051 138880 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3782049 138880 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
118465065 138850 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781574 138850 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
4106 2502 22 None -2 34 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
5358812 2502 22 None -2 34 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
89 2502 22 None -2 34 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
CHEMBL93240 2502 22 None -2 34 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
10470893 104968 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113361 104968 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
150 2509 21 None -2 16 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2509 21 None -2 16 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2509 21 None -2 16 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2509 21 None -2 16 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2509 21 None -2 16 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
118465026 138801 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780950 138801 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
9924293 68896 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL1922641 68896 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
118456745 138750 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780359 138750 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
73350387 89697 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89697 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
11333554 96661 22 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96661 22 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
44155994 57650 4 None - 1 Human 7.7 pIC50 = 7.7 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668571 57650 4 None - 1 Human 7.7 pIC50 = 7.7 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
3245407 48105 25 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 48105 25 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 72 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 72 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 72 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 72 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
22504458 104966 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113359 104966 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72197486 102503 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102503 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102503 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
124087 1389 114 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
49864530 15656 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222028 15656 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
3191 102858 97 None -15 25 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None -15 25 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
31101 729 40 None -23 36 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 729 40 None -23 36 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 729 40 None -23 36 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 729 40 None -23 36 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 729 40 None -23 36 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10427896 104956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113349 104956 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
72197485 102489 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393244 102489 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040288 102489 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
49799703 10992 4 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173577 10992 4 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
10885636 111016 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 111016 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44395664 66760 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
CHEMBL185850 66760 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
58149664 127423 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
CHEMBL3659970 127423 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
53322259 57652 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1668573 57652 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
9931929 63463 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
CHEMBL179814 63463 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
2286 3183 51 None -26 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 51 None -26 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 51 None -26 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 51 None -26 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 51 None -26 30 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
2398 954 62 None -5 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 62 None -5 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 62 None -5 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 62 None -5 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 62 None -5 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
44155992 57651 4 None - 1 Human 7.6 pIC50 = 7.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668572 57651 4 None - 1 Human 7.6 pIC50 = 7.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11725253 104965 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113358 104965 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72548703 161567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161567 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
53320009 56663 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56663 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
274 3339 44 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5312145 3339 44 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
CHEMBL433461 3339 44 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5 139 72 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 72 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 72 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 72 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
42388639 188054 0 None - 6 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
CHEMBL497749 188054 0 None - 6 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
2274 3173 58 None -23 31 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -23 31 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -23 31 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -23 31 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -23 31 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
1016 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 78 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
11743064 35953 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL144265 35953 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
49864599 15661 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccc(N2CCN(C)CC2)cc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222135 15661 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccc(N2CCN(C)CC2)cc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
5 139 72 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
5202 139 72 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
CHEMBL39 139 72 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
DB08839 139 72 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
2284 3182 33 None -12 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 33 None -12 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 33 None -12 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 33 None -12 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 33 None -12 29 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
1201549 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 597 24 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
133 2496 52 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 52 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 52 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 52 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 52 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
51003550 56665 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642118 56665 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
9998950 104972 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccc(Cl)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113365 104972 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccc(Cl)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
10247229 121046 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL356781 121046 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019508 10912 9 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172794 10912 9 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
90644511 111665 18 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 111665 18 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
277 1301 62 None -97 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 62 None -97 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 62 None -97 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 62 None -97 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 62 None -97 50 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
42635027 187397 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493625 187397 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
2162 41514 100 None -2 6 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41514 100 None -2 6 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
73356442 89696 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376485 89696 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
68303508 129763 5 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675192 129763 5 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
49864292 15595 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221452 15595 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
46934428 15660 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222134 15660 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
49864724 15692 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222364 15692 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
118465015 138741 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 7 1 5 3.7 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780252 138741 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 7 1 5 3.7 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
6918689 85984 4 None 812 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
CHEMBL23038 85984 4 None 812 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
10531 1420 21 None -9 23 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1420 21 None -9 23 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1420 21 None -9 23 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1420 21 None -9 23 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1420 21 None -9 23 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1042 1581 23 None -5 17 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1581 23 None -5 17 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1581 23 None -5 17 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1581 23 None -5 17 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1581 23 None -5 17 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
10020454 104999 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2c(C)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113559 104999 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2c(C)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019576 10897 6 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10897 6 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
118465055 138782 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 451 7 2 5 3.3 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780744 138782 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 451 7 2 5 3.3 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
44403358 70562 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 2 2 1 3.8 CCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194843 70562 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 2 2 1 3.8 CCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
44403375 71320 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 1 1 4.2 CCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL195759 71320 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 1 1 4.2 CCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
73347306 89694 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89694 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44155874 57620 22 None - 1 Human 7.5 pIC50 = 7.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57620 22 None - 1 Human 7.5 pIC50 = 7.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
72197668 102495 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393246 102495 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040325 102495 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
44403334 70310 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 258 3 2 2 3.2 CCc1[nH]c2ccc(OC)cc2c1C1CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194412 70310 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 258 3 2 2 3.2 CCc1[nH]c2ccc(OC)cc2c1C1CCNCC1 10.1016/j.bmcl.2005.06.067
4223 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 3992 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
68261572 129764 5 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675193 129764 5 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
3042 1414 35 None -51 14 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1414 35 None -51 14 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1414 35 None -51 14 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1414 35 None -51 14 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1414 35 None -51 14 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
2303 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3187 68 None -346 26 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4098 32505 30 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32505 30 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32505 30 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
118464990 138868 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781820 138868 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
56849714 68878 3 None - 1 Human 7.5 pIC50 = 7.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922623 68878 3 None - 1 Human 7.5 pIC50 = 7.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
49799667 10913 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10913 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
53326548 56662 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642115 56662 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
3158 56267 27 None -851 20 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 27 None -851 20 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
59636980 125837 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 377 5 0 7 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 nan
CHEMBL3648343 125837 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 377 5 0 7 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 nan
2247 505 81 None -53 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -53 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -53 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -53 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -53 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
76328541 105000 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 421 5 1 6 4.0 CSc1nc2c(Cc3ccccc3)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113560 105000 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 421 5 1 6 4.0 CSc1nc2c(Cc3ccccc3)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019553 10706 6 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10706 6 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322637 56671 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642124 56671 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
11162301 121016 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 297 4 1 6 1.7 CCCS(=O)(=O)c1c(SC)nc2ccccn2c1=N 10.1021/jm034142q
CHEMBL356540 121016 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 297 4 1 6 1.7 CCCS(=O)(=O)c1c(SC)nc2ccccn2c1=N 10.1021/jm034142q
44395451 66263 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184652 66263 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
72197484 102494 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102494 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102494 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
46885213 8460 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT6 (receptor)Inhibition of 5HT6 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8460 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT6 (receptor)Inhibition of 5HT6 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
49836386 18550 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
CHEMBL1275709 18550 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
2105 3054 37 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3054 37 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3054 37 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3054 37 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3054 37 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
156018343 177892 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3cc(NS(=O)(=O)c4cccc5ccccc45)ccc3s2)CC1 10.1016/j.ejmech.2018.11.017
CHEMBL4644799 177892 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3cc(NS(=O)(=O)c4cccc5ccccc45)ccc3s2)CC1 10.1016/j.ejmech.2018.11.017
10286610 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL355905 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
49864723 15691 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222363 15691 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
10286610 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL355905 120864 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
118465027 138852 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781617 138852 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
56849715 68879 3 None - 1 Human 8.4 pIC50 = 8.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922624 68879 3 None - 1 Human 8.4 pIC50 = 8.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44155874 57620 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57620 22 None - 1 Human 8.3 pIC50 = 8.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53324933 57622 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668502 57622 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
44403351 124196 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 286 1 1 1 4.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CC2CCC(C1)N2C 10.1016/j.bmcl.2005.06.067
CHEMBL363417 124196 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 286 1 1 1 4.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CC2CCC(C1)N2C 10.1016/j.bmcl.2005.06.067
9921064 127178 25 None - 3 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1016/j.bmcl.2005.06.067
CHEMBL365751 127178 25 None - 3 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1016/j.bmcl.2005.06.067
44403366 168469 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 3 2 1 4.2 CCCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL435126 168469 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 3 2 1 4.2 CCCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
21512050 89703 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 260 1 1 2 3.5 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1C 10.1016/j.ejmech.2013.03.006
CHEMBL2376492 89703 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 260 1 1 2 3.5 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1C 10.1016/j.ejmech.2013.03.006
3561 19077 39 None -3 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 19077 39 None -3 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
10427673 104997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2cc(C)ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113557 104997 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2cc(C)ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
53325266 56669 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 3 0 6 4.4 Cc1c(S(=O)(=O)N2CCC(=O)c3ccc(N4CCN(C)CC4)cc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.12.007
CHEMBL1642122 56669 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 3 0 6 4.4 Cc1c(S(=O)(=O)N2CCC(=O)c3ccc(N4CCN(C)CC4)cc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.12.007
107715 200945 22 None -29 19 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200945 22 None -29 19 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200945 22 None -29 19 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
53320011 56678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 CC1CC(=O)c2c(N3CCNCC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642131 56678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 CC1CC(=O)c2c(N3CCNCC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
10246904 104970 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 344 5 3 7 1.1 N=c1c(S(=O)(=O)c2ccccc2)c(NCCO)nc2ccccn12 10.1016/j.bmc.2014.01.003
CHEMBL3113363 104970 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 344 5 3 7 1.1 N=c1c(S(=O)(=O)c2ccccc2)c(NCCO)nc2ccccn12 10.1016/j.bmc.2014.01.003
10364512 104961 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 415 4 1 7 3.3 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113354 104961 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 415 4 1 7 3.3 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2014.01.003
49864600 15662 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 5.0 CC(C)N(c1ccc(Oc2cccnc2)nc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222136 15662 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 5.0 CC(C)N(c1ccc(Oc2cccnc2)nc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
11005810 10466 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10466 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
53325265 56666 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642119 56666 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
53318267 57656 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 nan
CHEMBL1668577 57656 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 nan
53326175 57659 4 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668580 57659 4 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
44476701 127421 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659968 127421 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
53317398 56676 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.7 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642129 56676 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.7 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
9929665 66791 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL185958 66791 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
10385670 104996 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 389 4 1 8 2.2 COC(=O)c1ccc2nc(SC)c(S(=O)(=O)c3ccccc3)c(=N)n2c1 10.1016/j.bmc.2014.01.003
CHEMBL3113556 104996 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 389 4 1 8 2.2 COC(=O)c1ccc2nc(SC)c(S(=O)(=O)c3ccccc3)c(=N)n2c1 10.1016/j.bmc.2014.01.003
44155871 60986 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762571 60986 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
16019580 10563 1 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10563 1 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118465046 138860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 481 8 2 6 3.3 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCNCC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781772 138860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 481 8 2 6 3.3 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCNCC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
53322935 57668 4 None - 1 Human 8.3 pIC50 = 8.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668589 57668 4 None - 1 Human 8.3 pIC50 = 8.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
118465021 138765 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780530 138765 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
58357860 129027 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670281 129027 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357805 129028 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 425 5 0 7 4.7 CSc1nn2c(C)c(Oc3ccccc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670282 129028 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 425 5 0 7 4.7 CSc1nn2c(C)c(Oc3ccccc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357740 129031 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3670285 129031 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
44403377 124840 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 302 4 1 1 5.0 CCCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL364271 124840 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 302 4 1 1 5.0 CCCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
73351903 89695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11741319 104960 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 393 3 1 6 3.6 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1cc(C)c(Cl)cc1C 10.1016/j.bmc.2014.01.003
CHEMBL3113353 104960 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 393 3 1 6 3.6 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1cc(C)c(Cl)cc1C 10.1016/j.bmc.2014.01.003
44155875 60983 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1762568 60983 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46700867 175990 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
CHEMBL4588956 175990 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
1472656 34628 25 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1429795 34628 25 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
1212 1662 50 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
10246185 104964 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 332 3 0 6 2.2 CSc1nc2ccccn2c(=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113357 104964 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 332 3 0 6 2.2 CSc1nc2ccccn2c(=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
11414926 34380 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 285 4 1 5 2.3 N#C/C(=C\Nc1ccccn1)S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL142783 34380 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 285 4 1 5 2.3 N#C/C(=C\Nc1ccccn1)S(=O)(=O)c1ccccc1 10.1021/jm034142q
8447 188949 84 None -33 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188949 84 None -33 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
6623 163321 98 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL418971 163321 98 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
10249280 37175 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL145304 37175 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
1971 2866 38 None -14 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 38 None -14 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 38 None -14 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 38 None -14 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 38 None -14 30 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
10409272 104993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 409 3 1 6 3.1 CSc1nc2ccc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113553 104993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 409 3 1 6 3.1 CSc1nc2ccc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
49799685 10951 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173209 10951 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
2726 919 68 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
10091305 105003 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 382 3 1 7 2.9 CSc1nc2c3ncccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113563 105003 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 382 3 1 7 2.9 CSc1nc2c3ncccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
53321319 56677 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 513 3 0 5 4.1 CN1CCN(c2cc(Br)cc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642130 56677 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 513 3 0 5 4.1 CN1CCN(c2cc(Br)cc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
10362440 121768 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2014.01.003
CHEMBL358948 121768 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2014.01.003
CHEMBL508338 188966 0 None -95 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
49864289 15592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221449 15592 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
7184883 10896 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10896 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
7185123 10677 6 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10677 6 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44403376 133580 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.6 CCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL371203 133580 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.6 CCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
10341241 104971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 405 4 2 7 3.4 Cc1ccc(Nc2nc3ccc(C)cn3c(=N)c2S(=O)(=O)c2ccccc2)nc1 10.1016/j.bmc.2014.01.003
CHEMBL3113364 104971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 405 4 2 7 3.4 Cc1ccc(Nc2nc3ccc(C)cn3c(=N)c2S(=O)(=O)c2ccccc2)nc1 10.1016/j.bmc.2014.01.003
10094519 105002 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 435 5 1 6 4.3 CSc1nc2c(C)cc(Cc3ccccc3)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113562 105002 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 435 5 1 6 4.3 CSc1nc2c(C)cc(Cc3ccccc3)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
44403386 70577 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 336 3 1 1 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL194908 70577 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 336 3 1 1 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.06.067
53320010 56664 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642117 56664 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
16019573 10994 10 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173579 10994 10 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
161 754 6 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 754 6 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 754 6 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
49864602 15664 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
CHEMBL1222138 15664 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
7184886 10606 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10606 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10452816 104959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 387 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113352 104959 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 387 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1016/j.bmc.2014.01.003
194 3507 31 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
443391 3507 31 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
CHEMBL14460 3507 31 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
10249280 37175 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL145304 37175 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
56849580 68875 5 None - 1 Human 7.2 pIC50 = 7.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922620 68875 5 None - 1 Human 7.2 pIC50 = 7.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
42635388 187698 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL495250 187698 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
49864722 15690 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1222362 15690 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
53325267 56672 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642125 56672 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
44476607 82352 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172192 82352 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
10131112 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
10131112 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1552 25 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
16019292 10993 7 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10993 7 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44403384 133275 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.5 CCc1[nH]c2ccc(Cl)cc2c1C1=CCN(CC)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL370436 133275 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.5 CCc1[nH]c2ccc(Cl)cc2c1C1=CCN(CC)CC1 10.1016/j.bmcl.2005.06.067
10021389 32936 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1021/jm034142q
CHEMBL141549 32936 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1021/jm034142q
73356443 89701 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376490 89701 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11740084 104998 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 5 1 6 3.3 CCCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
CHEMBL3113558 104998 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 5 1 6 3.3 CCCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
100 3805 58 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
45278805 7450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086754 7450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
191 403 98 None -20 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -20 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -20 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -20 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -20 29 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
58149665 82344 3 None - 1 Human 7.1 pIC50 = 7.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172183 82344 3 None - 1 Human 7.1 pIC50 = 7.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
42635387 187692 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495212 187692 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
26987 949 33 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 33 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 33 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 33 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 33 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
11730467 11028 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 11028 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
108029 3414 57 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
23 3414 57 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL18785 3414 57 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
10362440 121768 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm034142q
CHEMBL358948 121768 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm034142q
12147017 166058 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL425714 166058 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
51003551 56670 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642123 56670 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
44388701 123135 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL361213 123135 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
9976690 104995 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 374 4 2 7 1.5 CSc1nc2ccc(C(N)=O)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113555 104995 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 374 4 2 7 1.5 CSc1nc2ccc(C(N)=O)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
3066250 70286 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 70286 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
73351911 89705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 3 1 2 4.4 CCCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
CHEMBL2376560 89705 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 3 1 2 4.4 CCCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
10021389 32936 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
CHEMBL141549 32936 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
59636981 125836 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 361 4 0 6 3.6 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(C)cc1 nan
CHEMBL3648342 125836 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 361 4 0 6 3.6 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(C)cc1 nan
3066250 70286 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 70286 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
10907460 9828 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9828 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44476801 82349 3 None - 1 Human 6.1 pIC50 = 6.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172189 82349 3 None - 1 Human 6.1 pIC50 = 6.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
10090742 104963 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 3 0 6 2.3 CSc1nc2ccccn2/c(=N\C(C)=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113356 104963 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 3 0 6 2.3 CSc1nc2ccccn2/c(=N\C(C)=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
135 2532 43 None -21 58 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 43 None -21 58 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 43 None -21 58 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 43 None -21 58 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 43 None -21 58 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
12 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
12 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 1553 17 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
10247229 121046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL356781 121046 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
6758 167116 75 None - 1 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
CHEMBL429023 167116 75 None - 1 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
4011 82408 49 None -28 24 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 49 None -28 24 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
73354883 89699 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 349 4 2 4 4.6 Cc1[nH]c2ccc(Oc3ccccc3[N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376488 89699 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 349 4 2 4 4.6 Cc1[nH]c2ccc(Oc3ccccc3[N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
51003586 56673 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 4 0 5 4.2 CCC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642126 56673 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 4 0 5 4.2 CCC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
22424009 10954 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 5 1 8 3.4 CCC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173211 10954 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 5 1 8 3.4 CCC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44403335 70279 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 256 3 2 2 3.1 CCc1[nH]c2ccc(OC)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194248 70279 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 256 3 2 2 3.1 CCc1[nH]c2ccc(OC)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
45482789 198925 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 198925 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
20901207 10984 0 None - 1 Human 7.0 pIC50 = 7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10984 0 None - 1 Human 7.0 pIC50 = 7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
2303 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3187 68 None -346 26 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
6918689 85984 4 None 812 2 Human 8.5 pKd = 8.5 Binding
Antagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsAntagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
CHEMBL23038 85984 4 None 812 2 Human 8.5 pKd = 8.5 Binding
Antagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsAntagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
6918786 114168 1 None - 1 Human 10.4 pKi = 10.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 425 3 1 4 3.2 O=S(=O)(c1cccc(Cl)c1Cl)N1CCc2c(cccc2N2CCNCC2)C1 10.1021/jm5003952
CHEMBL3329438 114168 1 None - 1 Human 10.4 pKi = 10.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 425 3 1 4 3.2 O=S(=O)(c1cccc(Cl)c1Cl)N1CCc2c(cccc2N2CCNCC2)C1 10.1021/jm5003952
57412089 131776 0 None - 1 Human 10.3 pKi = 10.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692995 131776 0 None - 1 Human 10.3 pKi = 10.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
46889326 7015 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 340 3 2 3 3.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3c[nH]c4ccccc34)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084794 7015 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 340 3 2 3 3.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3c[nH]c4ccccc34)ccc21 10.1016/j.bmcl.2010.03.110
46889856 7170 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 329 4 0 3 3.5 CN(C)CC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085462 7170 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 329 4 0 3 3.5 CN(C)CC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
22557235 153571 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 3 1 5 3.0 O=S(=O)(c1c(Cl)cccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL398034 153571 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 3 1 5 3.0 O=S(=O)(c1c(Cl)cccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
46889893 7367 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 319 3 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086326 7367 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 319 3 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
68109141 131663 0 None - 1 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 3 2 5 3.4 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692882 131663 0 None - 1 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 3 2 5 3.4 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(oc12)CCNC3 nan
118181414 191195 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5189271 191195 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44156628 6714 4 None 2630 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6714 4 None 2630 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
164616201 184832 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 467 11 2 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4852099 184832 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 467 11 2 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113783
46890192 7095 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 5 2 4 2.2 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085120 7095 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 5 2 4 2.2 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890322 7216 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 1 4 2.8 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CC(O)C1 10.1016/j.bmcl.2010.03.110
CHEMBL1085658 7216 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 1 4 2.8 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CC(O)C1 10.1016/j.bmcl.2010.03.110
11654245 7318 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 401 4 2 5 2.2 O=C1CN=C(NC[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)N1 10.1016/j.bmcl.2010.03.110
CHEMBL1086113 7318 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 401 4 2 5 2.2 O=C1CN=C(NC[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)N1 10.1016/j.bmcl.2010.03.110
46889328 7347 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 6 2 4 2.2 NC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086252 7347 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 6 2 4 2.2 NC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10182243 130663 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL368209 130663 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
68115723 131771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(oc12)CCNC3 nan
CHEMBL3692990 131771 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(oc12)CCNC3 nan
57414386 131749 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692968 131749 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
68115821 131774 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 3 1 5 3.7 COc1cc(S(=O)(=O)c2cc(F)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692993 131774 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 3 1 5 3.7 COc1cc(S(=O)(=O)c2cc(F)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115733 132253 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 1 5 3.3 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696966 132253 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 1 5 3.3 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44156754 6510 4 None 891 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6510 4 None 891 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
10982183 93220 0 None 177 3 Human 9.9 pKi = 9.9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 396 3 2 6 1.7 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCNCC3)c2)cc1 10.1021/jm021085c
CHEMBL24474 93220 0 None 177 3 Human 9.9 pKi = 9.9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 396 3 2 6 1.7 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCNCC3)c2)cc1 10.1021/jm021085c
68109407 131647 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 1 5 2.9 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692867 131647 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 1 5 2.9 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44398571 124370 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 382 4 0 5 3.4 CON1CCN(c2ccc(S(=O)(=O)c3cccc4ccccc34)cc2)CC1 10.1021/jm050247c
CHEMBL363792 124370 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 382 4 0 5 3.4 CON1CCN(c2ccc(S(=O)(=O)c3cccc4ccccc34)cc2)CC1 10.1021/jm050247c
6918745 127049 2 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 341 3 2 4 2.4 O=S(=O)(c1ccccc1)c1cc2c(N3CCNCC3)cccc2[nH]1 10.1021/jm050247c
CHEMBL365569 127049 2 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 341 3 2 4 2.4 O=S(=O)(c1ccccc1)c1cc2c(N3CCNCC3)cccc2[nH]1 10.1021/jm050247c
46890190 6802 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083886 6802 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890264 6996 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 398 5 2 4 1.9 NS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084711 6996 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 398 5 2 4 1.9 NS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889350 7083 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 363 6 2 4 2.7 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
CHEMBL1085037 7083 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 363 6 2 4 2.7 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
68115629 131691 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 2 4 4.0 O=S(=O)(c1ccc2[nH]ccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692910 131691 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 2 4 4.0 O=S(=O)(c1ccc2[nH]ccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116227 131755 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692974 131755 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
68108832 131675 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131675 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
46890324 6908 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 381 6 2 4 2.8 O=S(=O)(c1cccc(F)c1)c1cc(F)c2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
CHEMBL1084336 6908 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 381 6 2 4 2.8 O=S(=O)(c1cccc(F)c1)c1cc(F)c2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
46890884 7192 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085585 7192 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889918 7200 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 4 2 3 2.5 CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085617 7200 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 4 2 3 2.5 CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
11595360 7309 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 343 4 3 3 2.4 N=C(N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086079 7309 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 343 4 3 3 2.4 N=C(N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46889890 7364 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 301 3 1 3 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086323 7364 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 301 3 1 3 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
22557241 149584 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 6 1.8 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL394690 149584 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 6 1.8 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
68115724 131769 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 3 1 6 3.4 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(oc12)CCNC3 nan
CHEMBL3692988 131769 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 3 1 6 3.4 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(oc12)CCNC3 nan
68115722 131770 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692989 131770 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
11256720 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
9444 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
CHEMBL1083390 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
DB12680 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
11256720 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
9444 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
CHEMBL1083390 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
DB12680 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
68108708 131643 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 400 2 1 5 4.1 Cn1cc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
CHEMBL3692863 131643 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 400 2 1 5 4.1 Cn1cc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
68115667 131778 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2cccs2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692997 131778 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2cccs2)cc2c3c(oc12)CCNC3 nan
118173772 190375 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5177311 190375 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115716 131752 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
CHEMBL3692971 131752 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
68116278 131756 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692975 131756 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
24873459 135534 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 399 5 3 3 4.3 NCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm050247c
CHEMBL372879 135534 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 399 5 3 3 4.3 NCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm050247c
44398389 136256 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 429 3 0 5 4.4 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4C=CCC4C3)cc21 10.1021/jm050247c
CHEMBL373322 136256 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 429 3 0 5 4.4 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4C=CCC4C3)cc21 10.1021/jm050247c
46220503 6457 13 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 362 4 2 3 2.7 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082508 6457 13 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 362 4 2 3 2.7 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
11639865 6755 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 397 5 1 4 2.6 CS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083781 6755 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 397 5 1 4 2.6 CS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890325 6976 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 380 4 2 3 2.9 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1084603 6976 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 380 4 2 3 2.9 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
6918751 114160 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 2 4 3.7 O=S(=O)(c1cc2cccc(N3CCNCC3)c2[nH]1)c1cccc(Cl)c1Cl 10.1021/jm5003952
CHEMBL3329430 114160 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 2 4 3.7 O=S(=O)(c1cc2cccc(N3CCNCC3)c2[nH]1)c1cccc(Cl)c1Cl 10.1021/jm5003952
11652654 114172 0 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 4 1 5 1.9 CNC[C@@H]1COc2ccc(S(=O)(=O)c3ccccc3)cc2O1 10.1021/jm5003952
CHEMBL3329442 114172 0 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 4 1 5 1.9 CNC[C@@H]1COc2ccc(S(=O)(=O)c3ccccc3)cc2O1 10.1021/jm5003952
10019089 114181 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 323 3 1 4 2.0 O=C1COc2c(N3CCNCC3)cccc2N1Cc1ccccc1 10.1021/jm5003952
CHEMBL3329451 114181 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 323 3 1 4 2.0 O=C1COc2c(N3CCNCC3)cccc2N1Cc1ccccc1 10.1021/jm5003952
145954675 162678 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 362 3 1 3 3.0 CN(C(N)=O)[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4170220 162678 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 362 3 1 3 3.0 CN(C(N)=O)[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.ejmech.2017.12.053
6918715 91923 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrsDisplacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrs
ChEMBL 407 3 1 5 2.6 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1Cl)CCO2 10.1016/j.bmc.2013.05.040
CHEMBL2413982 91923 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrsDisplacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrs
ChEMBL 407 3 1 5 2.6 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1Cl)CCO2 10.1016/j.bmc.2013.05.040
9910619 176917 9 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL46187 176917 9 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
44516817 57663 5 None 4365 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57663 5 None 4365 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
6918836 60541 16 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm049615n
CHEMBL175835 60541 16 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm049615n
68108410 131644 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 1 5 3.9 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
CHEMBL3692864 131644 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 1 5 3.9 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
68115714 131754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692973 131754 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
44156752 6580 4 None 645 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6580 4 None 645 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
118181460 189893 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5169546 189893 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
72549033 110693 0 None 562 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260311 110693 0 None 562 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
68109211 131646 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692866 131646 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
68116231 132240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.2 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696953 132240 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.2 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
68115666 131777 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 4.2 COc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692996 131777 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 4.2 COc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115858 132243 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 5 4.4 Cc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696956 132243 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 5 4.4 Cc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
11256720 2055 79 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
9444 2055 79 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
CHEMBL1083390 2055 79 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
DB12680 2055 79 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
53323402 60142 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642864 60142 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739646 60142 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
46780481 107531 20 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
9903970 107531 20 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
CHEMBL3187365 107531 20 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
CHEMBL3544974 107531 20 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
68109588 131682 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CCNCC3 nan
CHEMBL3692901 131682 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CCNCC3 nan
46890326 6977 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 395 5 2 4 2.3 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1084604 6977 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 395 5 2 4 2.3 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
46889351 7084 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 7 1 4 3.3 COCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085038 7084 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 7 1 4 3.3 COCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889891 7365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 317 3 2 4 2.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(O)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086324 7365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 317 3 2 4 2.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(O)c3)ccc21 10.1016/j.bmcl.2010.03.110
10270854 71675 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196410 71675 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
46867521 6509 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082762 6509 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
58258774 128973 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128973 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
118181454 189961 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5170650 189961 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
118173755 192334 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206617 192334 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44327759 207912 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL96745 207912 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115757 131723 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1csc2ccccc12 nan
CHEMBL3692942 131723 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1csc2ccccc12 nan
68115754 131773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccsc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692992 131773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccsc2)cc2c3c(oc12)CCNC3 nan
52914691 70773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
57394334 70774 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950776 70774 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
11256720 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2055 79 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
52914691 70773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70773 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57394334 70774 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70774 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115840 131775 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692994 131775 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
68115738 131781 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3693000 131781 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
58258777 128980 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 2 1 5 4.9 Cc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669657 128980 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 2 1 5 4.9 Cc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
10027190 120402 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 458 7 0 7 3.9 COc1ccc(OC)c(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)c1 10.1016/j.bmcl.2004.01.071
CHEMBL353552 120402 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 458 7 0 7 3.9 COc1ccc(OC)c(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)c1 10.1016/j.bmcl.2004.01.071
9822810 69502 0 None 6 2 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1021/jm5003952
CHEMBL193400 69502 0 None 6 2 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1021/jm5003952
11569025 114182 1 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 471 3 1 4 5.2 O=C1c2cccc(N3CCNCC3)c2Oc2ccc(F)cc2N1Cc1cccc(C(F)(F)F)c1 10.1021/jm5003952
CHEMBL3329452 114182 1 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 471 3 1 4 5.2 O=C1c2cccc(N3CCNCC3)c2Oc2ccc(F)cc2N1Cc1cccc(C(F)(F)F)c1 10.1021/jm5003952
11587610 114183 3 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 3 2 4 1.8 O=c1[nH]c2c(N3CCNCC3)cccc2n1Cc1ccccc1 10.1021/jm5003952
CHEMBL3329453 114183 3 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 3 2 4 1.8 O=c1[nH]c2c(N3CCNCC3)cccc2n1Cc1ccccc1 10.1021/jm5003952
11624561 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL187865 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL194307 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
9840981 162650 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4169827 162650 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
44327759 207912 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1021/jm030030n
CHEMBL96745 207912 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1021/jm030030n
10154392 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL370779 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2020.112765
4106 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
5358812 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
89 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
CHEMBL93240 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
10154392 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL370779 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2016.08.016
4106 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
5358812 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
89 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
CHEMBL93240 2502 22 None -2 34 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
164610804 185087 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 9 2 6 4.0 CC(=O)Nc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4855991 185087 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 9 2 6 4.0 CC(=O)Nc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
11624561 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL187865 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL194307 70287 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
9950255 196815 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565723 196815 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9956634 63486 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 475 8 2 4 6.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
CHEMBL179926 63486 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 475 8 2 4 6.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
11363934 202243 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
CHEMBL609994 202243 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
118010064 132241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 5 3.8 Cc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696954 132241 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 5 3.8 Cc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
58258781 128984 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 2 5 3.9 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669661 128984 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 2 5 3.9 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258821 129010 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669687 129010 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
17940125 120908 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL356021 120908 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10413595 161841 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161841 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10413595 161841 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1021/jm050247c
CHEMBL414628 161841 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1021/jm050247c
11682024 6518 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1082777 6518 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)cc(F)c21 10.1016/j.bmcl.2010.03.110
11515192 7091 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.2 CNCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085111 7091 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.2 CNCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46889917 7152 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 290 3 2 3 2.2 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085372 7152 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 290 3 2 3 2.2 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
46889353 7392 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 5 2 4 2.2 NCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086477 7392 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 5 2 4 2.2 NCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
17978373 69812 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)ccc(Cl)c21 10.1016/j.bmcl.2005.06.107
CHEMBL193629 69812 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)ccc(Cl)c21 10.1016/j.bmcl.2005.06.107
10154392 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL370779 133516 11 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
17978408 133619 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371375 133619 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
10134086 165910 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 2 4 3.1 O=S(=O)(c1cccc(Cl)c1)c1c[nH]c2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL425015 165910 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 2 4 3.1 O=S(=O)(c1cccc(Cl)c1)c1c[nH]c2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
11407072 93672 1 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 405 3 1 5 2.6 CC1(C)CN(S(=O)(=O)c2ccccc2F)c2cccc(N3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL246918 93672 1 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 405 3 1 5 2.6 CC1(C)CN(S(=O)(=O)c2ccccc2F)c2cccc(N3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
52914691 70773 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70773 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
52914691 70773 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70773 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115828 131750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692969 131750 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
68115806 131766 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 441 4 2 6 3.5 COc1cc(S(=O)(=O)c2cccc(C(O)C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692985 131766 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 441 4 2 6 3.5 COc1cc(S(=O)(=O)c2cccc(C(O)C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
58258771 128963 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 2 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669640 128963 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 2 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
118181455 191065 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5187350 191065 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
57394334 70774 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70774 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115726 131772 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692991 131772 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
68115779 132254 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 4 1 5 3.5 O=S(=O)(c1ccccc1)c1cc(OC(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696967 132254 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 4 1 5 3.5 O=S(=O)(c1ccccc1)c1cc(OC(F)F)c2oc3c(c2c1)CNCC3 nan
10172764 110694 10 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260313 110694 10 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
CHEMBL5201619 110694 10 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
58258774 128973 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128973 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258788 129013 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669690 129013 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
68108997 131639 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cccc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692859 131639 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cccc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68108832 131675 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131675 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
68115721 131765 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(C(C)(C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692984 131765 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(C(C)(C)O)c2)cc2c3c(oc12)CCNC3 nan
57394334 70774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950776 70774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
57394334 70774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115660 131767 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131767 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
52914691 70773 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70773 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
52914691 70773 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70773 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44476436 82347 6 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172186 82347 6 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
44476436 82347 6 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 82347 6 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
68108513 131640 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692860 131640 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115756 131780 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
CHEMBL3692999 131780 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
46890157 6458 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 2 3 3.0 CNC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082509 6458 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 2 3 3.0 CNC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890221 6756 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 411 5 0 4 3.0 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(C)(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1083782 6756 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 411 5 0 4 3.0 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(C)(=O)=O 10.1016/j.bmcl.2010.03.110
46890155 6852 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 404 6 1 4 2.8 CN(C)CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084071 6852 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 404 6 1 4 2.8 CN(C)CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889892 7366 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 2.9 COc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1086325 7366 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 2.9 COc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
10156341 135245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL372513 135245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
44403305 135613 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.107
CHEMBL372929 135613 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.107
17960999 93574 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 391 3 1 5 2.1 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246499 93574 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 391 3 1 5 2.1 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
11697242 93623 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 3 1 5 2.5 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246705 93623 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 3 1 5 2.5 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
22557272 93624 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 389 4 1 6 1.7 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246706 93624 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 389 4 1 6 1.7 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
11631819 114171 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)OCCC2N1CCNCC1 10.1021/jm5003952
CHEMBL3329441 114171 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)OCCC2N1CCNCC1 10.1021/jm5003952
44389003 123836 0 None 954 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362487 123836 0 None 954 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46227395 200129 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL596199 200129 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
4106 2502 22 None -2 34 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2502 22 None -2 34 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2502 22 None -2 34 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2502 22 None -2 34 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
164611660 184738 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccn3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4850738 184738 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccn3)cccc21 10.1016/j.ejmech.2021.113792
11566597 72995 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 3 2 6 1.9 Nc1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL200795 72995 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 3 2 6 1.9 Nc1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2005.08.059
71151933 118240 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 558 9 1 7 4.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409238 118240 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 558 9 1 7 4.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
10112810 63339 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 7 2 3 4.7 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
CHEMBL179408 63339 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 7 2 3 4.7 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
11384146 201733 0 None 6 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 201733 0 None 6 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
11351089 201736 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606559 201736 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
118010063 124460 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2ccc(OC(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3639918 124460 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2ccc(OC(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115868 132249 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 2 1 6 3.3 Cn1cc(S(=O)(=O)c2cc(C#N)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
CHEMBL3696962 132249 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 2 1 6 3.3 Cn1cc(S(=O)(=O)c2cc(C#N)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
57403058 70775 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL1950777 70775 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
68115660 131767 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131767 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
58258772 127944 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127944 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258774 128973 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128973 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
68109265 131636 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 366 2 1 5 3.6 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)c2ccccc12 nan
CHEMBL3692856 131636 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 366 2 1 5 3.6 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)c2ccccc12 nan
58258763 129012 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669689 129012 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
118654432 191480 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5193483 191480 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
118173792 192418 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5208122 192418 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
155557005 174533 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4555868 174533 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
44155109 8174 4 None - 1 Human 9.4 pKi = 9.4 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8174 4 None - 1 Human 9.4 pKi = 9.4 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44155109 8174 4 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8174 4 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
44156863 8078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 8078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
44156863 8078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 8078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
58258753 129004 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669681 129004 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
118654422 192325 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5206470 192325 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
118181441 192291 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206037 192291 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
58258878 128962 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 2 2 4 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(C(F)(F)F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669639 128962 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 2 2 4 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(C(F)(F)F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
58258780 128978 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 2 1 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)cc(F)c31)C1CCC(C2)N1 nan
CHEMBL3669655 128978 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 2 1 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)cc(F)c31)C1CCC(C2)N1 nan
68109652 131638 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692858 131638 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115692 131747 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)CCOC3)cc2c3c(oc12)CCNC3 nan
CHEMBL3692966 131747 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)CCOC3)cc2c3c(oc12)CCNC3 nan
44156756 6581 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1083076 6581 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
68116229 131751 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2ccc(C(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692970 131751 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2ccc(C(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115660 131767 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131767 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
46867519 6508 4 None 331 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6508 4 None 331 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
6918682 114159 32 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 355 3 1 4 2.8 CN1CCN(c2cccc3c(S(=O)(=O)c4ccccc4)c[nH]c23)CC1 10.1021/jm5003952
CHEMBL3329429 114159 32 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 355 3 1 4 2.8 CN1CCN(c2cccc3c(S(=O)(=O)c4ccccc4)c[nH]c23)CC1 10.1021/jm5003952
10178788 135251 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1021/jm5003952
CHEMBL372537 135251 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1021/jm5003952
58258778 127927 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127927 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
58258755 128997 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669674 128997 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
58258797 129005 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669682 129005 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
134131472 142178 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.bmcl.2021.127909
CHEMBL3883955 142178 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.bmcl.2021.127909
46203710 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL3329435 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
164625599 185759 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 10 1 7 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1OC 10.1016/j.ejmech.2021.113792
CHEMBL4866390 185759 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 10 1 7 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1OC 10.1016/j.ejmech.2021.113792
164622030 186098 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 8 1 7 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc4c(c3)OCCO4)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4871652 186098 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 8 1 7 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc4c(c3)OCCO4)cccc21 10.1016/j.ejmech.2021.113792
23624307 192406 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520795 192406 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
134131472 142178 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.ejmech.2016.09.008
CHEMBL3883955 142178 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.ejmech.2016.09.008
10278839 63338 0 None - 1 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 503 10 2 4 6.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
CHEMBL179407 63338 0 None - 1 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 503 10 2 4 6.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
68115836 132239 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696952 132239 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
18354536 48603 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155717 48603 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940169 50586 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3c(Cl)ccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157454 50586 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3c(Cl)ccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940215 119599 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2cccc(I)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346338 119599 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2cccc(I)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9889681 208063 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 208063 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
9889681 208063 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 208063 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
46889895 7151 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 324 3 1 4 3.5 N#Cc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3C=N)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085368 7151 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 324 3 1 4 3.5 N#Cc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3C=N)c1 10.1016/j.bmcl.2010.03.110
44403327 70579 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 6 2.3 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL194915 70579 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 6 2.3 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10178788 135251 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL372537 135251 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
20765669 93511 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 8 1.9 O=S(=O)(c1cccc2nonc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246291 93511 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 8 1.9 O=S(=O)(c1cccc2nonc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
168285508 191676 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 373 3 1 5 2.7 Cc1cn(S(=O)(=O)c2cccc(F)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmc.2022.116950
CHEMBL5196479 191676 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 373 3 1 5 2.7 Cc1cn(S(=O)(=O)c2cccc(F)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmc.2022.116950
25117676 200459 0 None 831 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 200459 0 None 831 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
118654426 190989 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5186310 190989 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
46203710 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL3329435 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258769 129001 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 129001 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258817 129008 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669685 129008 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
46203710 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2021.128275
CHEMBL3329435 114165 4 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2021.128275
44155107 8079 4 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 8079 4 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44155107 8079 4 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 8079 4 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
118181437 192113 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5203370 192113 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68109001 131637 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692857 131637 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414668 131724 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1ccc2sccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692943 131724 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1ccc2sccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58258837 128979 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 2 1 5 4.2 Cc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669656 128979 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 2 1 5 4.2 Cc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258776 129006 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669683 129006 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258836 127943 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127943 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258802 129014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669691 129014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
10202564 1524 14 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
3217 1524 14 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
CHEMBL362628 1524 14 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
68109317 131634 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 352 2 1 5 3.3 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
CHEMBL3692854 131634 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 352 2 1 5 3.3 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
58258778 127927 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127927 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
11465618 102398 23 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 102398 23 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 102398 23 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
68115815 132271 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 358 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCC(O)C3 nan
CHEMBL3696984 132271 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 358 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCC(O)C3 nan
23844114 207517 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.05.076
CHEMBL94569 207517 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.05.076
23872164 9545 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 371 7 1 5 3.3 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL112296 9545 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 371 7 1 5 3.3 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
6918648 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm030030n
CHEMBL29846 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm030030n
10250472 111352 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 401 8 1 6 3.4 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL326937 111352 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 401 8 1 6 3.4 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
16117153 60139 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 60139 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 60139 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
9802776 101756 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL299822 101756 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
25263305 184218 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 3.6 Cc1c(OCc2cccc(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483358 184218 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 3.6 Cc1c(OCc2cccc(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
68115787 131761 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc(C(C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692980 131761 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc(C(C)O)c2)cc2c3c(oc12)CCNC3 nan
46224879 201547 3 None -2 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 201547 3 None -2 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
46889858 7093 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2021.128275
CHEMBL1085113 7093 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2021.128275
9954121 96406 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL261917 96406 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
17940212 119458 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL345110 119458 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918648 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
6918648 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL29846 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/j.bmcl.2010.12.007
9954121 96406 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL261917 96406 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
276 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
5312149 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
CHEMBL431298 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
46890156 6695 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 389 4 3 4 2.5 N=C(N)NC(=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083575 6695 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 389 4 3 4 2.5 N=C(N)NC(=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889858 7093 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085113 7093 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46890295 7212 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 416 5 2 4 2.9 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)[C@H]1CCCN1 10.1016/j.bmcl.2010.03.110
CHEMBL1085651 7212 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 416 5 2 4 2.9 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)[C@H]1CCCN1 10.1016/j.bmcl.2010.03.110
11688736 7311 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 342 4 2 3 3.5 CC(=N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086080 7311 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 342 4 2 3 3.5 CC(=N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
44403304 70152 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmcl.2005.06.107
CHEMBL194039 70152 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmcl.2005.06.107
20765664 93573 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 444 3 1 6 2.9 O=S(=O)(c1cccc2cccnc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246498 93573 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 444 3 1 6 2.9 O=S(=O)(c1cccc2cccnc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
17961002 93622 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 3 1 5 2.0 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(F)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246704 93622 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 3 1 5 2.0 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(F)cc21 10.1016/j.bmcl.2006.12.093
11200890 149588 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 3 1 5 2.7 O=S(=O)(c1ccccc1F)N1CC2(CCC2)Oc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL394691 149588 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 3 1 5 2.7 O=S(=O)(c1ccccc1F)N1CC2(CCC2)Oc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
6918648 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 101559 1 None 323 14 Human 9.2 pKi = 9.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
118181453 191552 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5194574 191552 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
276 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
5312149 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
CHEMBL431298 3513 50 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
70245924 82353 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172193 82353 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
68115709 131746 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 3 1 4 4.6 C=C(C)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692965 131746 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 3 1 4 4.6 C=C(C)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
70245924 82353 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172193 82353 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
118173790 191985 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5201308 191985 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
46830134 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmc.2013.05.040
CHEMBL1092241 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmc.2013.05.040
57403057 70771 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70771 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
58258868 129009 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 3 0 5 3.7 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669686 129009 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 3 0 5 3.7 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1C nan
46830134 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
118654354 190012 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5171470 190012 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
46830134 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8217 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
57403057 70771 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70771 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44476514 82348 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172187 82348 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
44476514 82348 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172187 82348 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
58258810 129000 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669677 129000 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
68115710 131762 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692981 131762 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
3241 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
6918649 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
CHEMBL1210710 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
6918836 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
CHEMBL175835 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
9910619 176917 9 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1021/jm030030n
CHEMBL46187 176917 9 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1021/jm030030n
16118795 60096 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 60096 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 60096 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
3241 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918649 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
CHEMBL1210710 3521 24 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918836 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmcl.2007.09.016
CHEMBL175835 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmcl.2007.09.016
44433196 88722 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236104 88722 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44433198 147113 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392746 147113 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
6918836 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
CHEMBL175835 60541 16 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
9979611 16662 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 1 8 3.2 O=S(=O)(c1cn(C2CCCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
CHEMBL1242425 16662 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 1 8 3.2 O=S(=O)(c1cn(C2CCCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
52945783 16668 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 449 4 0 8 3.9 CCN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242518 16668 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 449 4 0 8 3.9 CCN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258787 127955 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 5 5.4 Cn1c2c(c3cc(S(=O)(=O)c4cn(Cc5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664780 127955 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 5 5.4 Cn1c2c(c3cc(S(=O)(=O)c4cn(Cc5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127930 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127930 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258808 127962 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL3664787 127962 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
3241 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
6918649 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
CHEMBL1210710 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
11393666 192986 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192986 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192986 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
57394333 70772 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70772 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
57394333 70772 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70772 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115659 131764 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2ccc(C(C)(C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692983 131764 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2ccc(C(C)(C)O)cc2)cc2c3c(oc12)CCNC3 nan
58258758 128966 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128966 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
53303985 111692 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286585 111692 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
68115702 131757 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692976 131757 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
53303985 111692 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286585 111692 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
58258757 128996 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669673 128996 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
68115637 131690 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1Cl nan
CHEMBL3692909 131690 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1Cl nan
3241 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
6918649 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
CHEMBL1210710 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
196129 67798 17 None 1 15 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67798 17 None 1 15 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
10172764 110694 10 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL3260313 110694 10 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5201619 110694 10 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
57414524 131697 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692916 131697 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
44369415 43968 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 401 4 1 5 2.6 COc1ccc(S(=O)(=O)N2c3ccccc3CC2(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL151295 43968 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 401 4 1 5 2.6 COc1ccc(S(=O)(=O)N2c3ccccc3CC2(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354548 44573 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.6 COc1ccc(S(=O)(=O)N2CCCc3c(Cl)cc(Cl)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL151998 44573 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.6 COc1ccc(S(=O)(=O)N2CCCc3c(Cl)cc(Cl)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940101 46898 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(I)ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154089 46898 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(I)ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10837078 202822 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 445 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2ccc3c(Cl)cccc3c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62368 202822 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 445 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2ccc3c(Cl)cccc3c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10648664 202857 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62538 202857 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
9935387 99442 0 None 158 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1021/jm050247c
CHEMBL282971 99442 0 None 158 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1021/jm050247c
9913554 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm050247c
CHEMBL29433 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm050247c
9802776 101756 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1021/jm050247c
CHEMBL299822 101756 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1021/jm050247c
18180191 166306 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCNCC1 10.1021/jm050247c
CHEMBL427155 166306 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCNCC1 10.1021/jm050247c
44398325 168274 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm050247c
CHEMBL433946 168274 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm050247c
52946846 16683 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 0 8 3.1 CN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242703 16683 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 0 8 3.1 CN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
46890218 6911 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 391 6 1 4 2.8 COCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084358 6911 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 391 6 1 4 2.8 COCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889325 7014 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 308 3 1 5 2.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cncs3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084793 7014 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 308 3 1 5 2.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cncs3)ccc21 10.1016/j.bmcl.2010.03.110
11503175 153573 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 443 3 1 5 3.5 O=S(=O)(c1cccc2ccccc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL398036 153573 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 443 3 1 5 3.5 O=S(=O)(c1cccc2ccccc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
9935387 99442 0 None 158 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 99442 0 None 158 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
3241 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
6918649 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
CHEMBL1210710 3521 24 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
9913554 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm5003952
CHEMBL29433 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm5003952
58258769 129001 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 129001 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
23757270 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
CHEMBL94093 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
16037746 78281 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 332 4 1 6 2.5 COc1cc(OC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
CHEMBL210733 78281 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 332 4 1 6 2.5 COc1cc(OC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
9913554 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm030030n
CHEMBL29433 100992 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm030030n
23757270 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
23757270 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL94093 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL94093 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
23757270 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL94093 207435 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
16117283 60148 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1642883 60148 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1739658 60148 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
44433194 146602 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392318 146602 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9802776 101756 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL299822 101756 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
276 3513 50 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
5312149 3513 50 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
CHEMBL431298 3513 50 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
10157412 130699 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 2 3 4.2 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL368390 130699 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 2 3 4.2 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
68115671 131779 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 385 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)COC3)cc2c3c(oc12)CCNC3 nan
CHEMBL3692998 131779 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 385 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)COC3)cc2c3c(oc12)CCNC3 nan
57403058 70775 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL1950777 70775 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
57403058 70775 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 10.1016/j.bmcl.2012.01.022
CHEMBL1950777 70775 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 10.1016/j.bmcl.2012.01.022
44476607 82352 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172192 82352 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2023.117256
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2023.117256
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2023.117256
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2023.117256
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
21071390 1987 53 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
8689 1987 53 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
CHEMBL3286580 1987 53 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
DB11957 1987 53 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
118173771 191996 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5201491 191996 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
57403057 70771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
58258763 129012 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669689 129012 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258788 129013 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669690 129013 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
46889472 6889 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 383 3 1 7 1.5 O=S(=O)(c1ccccc1)c1cnn2c(N3CCNCC3)c3c(nc12)CCC3 10.1021/jm100350r
CHEMBL1084244 6889 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 383 3 1 7 1.5 O=S(=O)(c1ccccc1)c1cnn2c(N3CCNCC3)c3c(nc12)CCC3 10.1021/jm100350r
57403057 70771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
58258755 128997 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669674 128997 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
118173750 190791 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5183606 190791 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115873 132252 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 397 3 1 5 3.8 O=S(=O)(c1ccccc1)c1cc(OC(F)(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696965 132252 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 397 3 1 5 3.8 O=S(=O)(c1ccccc1)c1cc(OC(F)(F)F)c2oc3c(c2c1)CNCC3 nan
44435621 88784 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236336 88784 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
118712409 114180 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 379 5 1 6 2.5 COc1cc(Cn2c(=O)ccc3cccc(OC)c32)cc(N2CCNCC2)c1 10.1021/jm5003952
CHEMBL3329450 114180 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 379 5 1 6 2.5 COc1cc(Cn2c(=O)ccc3cccc(OC)c32)cc(N2CCNCC2)c1 10.1021/jm5003952
11326086 12767 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1187925 12767 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL534472 12767 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
10319296 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.05.076
CHEMBL443796 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.05.076
10319296 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00453-4
CHEMBL443796 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00453-4
10319296 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm030030n
CHEMBL443796 169702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm030030n
44435621 88784 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236336 88784 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45484333 196816 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565724 196816 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
45484340 196826 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565746 196826 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
49836620 18654 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276925 18654 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
4106 2502 22 None -2 34 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
5358812 2502 22 None -2 34 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
89 2502 22 None -2 34 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
CHEMBL93240 2502 22 None -2 34 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
58258810 129000 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669677 129000 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
70301391 114176 0 None - 1 Human 9.0 pKi = 9.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 312 4 1 2 4.5 CN1CCCC1Cc1c[nH]c2ccc(OC3CCCCC3)cc12 10.1021/jm5003952
CHEMBL3329446 114176 0 None - 1 Human 9.0 pKi = 9.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 312 4 1 2 4.5 CN1CCCC1Cc1c[nH]c2ccc(OC3CCCCC3)cc12 10.1021/jm5003952
4106 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
5358812 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
89 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
CHEMBL93240 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
1043 1582 14 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1582 14 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1582 14 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1582 14 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1582 14 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
58258764 127939 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127939 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258836 127943 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127943 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
4106 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
5358812 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
89 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
CHEMBL93240 2502 22 None -2 34 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
168298034 192738 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassayDisplacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassay
ChEMBL 445 6 2 6 3.2 COc1cc(NS(=O)(=O)c2ccc(OC)c(N3CCNCC3)c2)c(Cl)cc1Cl 10.1016/j.bmcl.2021.128275
CHEMBL5220473 192738 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassayDisplacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassay
ChEMBL 445 6 2 6 3.2 COc1cc(NS(=O)(=O)c2ccc(OC)c(N3CCNCC3)c2)c(Cl)cc1Cl 10.1016/j.bmcl.2021.128275
58258798 129007 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669684 129007 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
9931929 63463 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
CHEMBL179814 63463 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
6918689 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
CHEMBL23038 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
118712405 114162 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 4 0 5 4.0 CN1CCC(c2cn(C)c3cc(OS(=O)(=O)c4c(F)cccc4F)ccc23)CC1 10.1021/jm5003952
CHEMBL3329432 114162 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 4 0 5 4.0 CN1CCC(c2cn(C)c3cc(OS(=O)(=O)c4c(F)cccc4F)ccc23)CC1 10.1021/jm5003952
11164580 114170 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 4 2 4 3.3 O=S(=O)(Nc1ccc2c(c1)C(C1CCNCC1)=CCO2)c1ccccc1 10.1021/jm5003952
CHEMBL3329440 114170 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 4 2 4 3.3 O=S(=O)(Nc1ccc2c(c1)C(C1CCNCC1)=CCO2)c1ccccc1 10.1021/jm5003952
59017478 114179 3 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 349 4 1 5 3.8 COc1cc(N2CCNCC2)c2ncc(C)c(Oc3ccccc3)c2c1 10.1021/jm5003952
CHEMBL3329449 114179 3 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 349 4 1 5 3.8 COc1cc(N2CCNCC2)c2ncc(C)c(Oc3ccccc3)c2c1 10.1021/jm5003952
58258772 127944 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127944 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258822 129002 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669679 129002 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
58258817 129008 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669685 129008 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
276 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
5312149 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
CHEMBL431298 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
44388943 63290 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL179277 63290 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44389016 63920 0 None 741 3 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180606 63920 0 None 741 3 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44389015 122330 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359876 122330 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44389004 123126 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL361180 123126 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
10346043 47120 0 None 1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154274 47120 0 None 1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940224 47622 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 389 6 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccccc2C(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154675 47622 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 389 6 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccccc2C(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9891618 107124 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 107124 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 107408 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 107408 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
9890119 208057 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 208057 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
10505579 100579 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 501 5 1 5 3.2 COc1ccc(NS(=O)(=O)c2cc(I)ccc2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL291618 100579 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 501 5 1 5 3.2 COc1ccc(NS(=O)(=O)c2cc(I)ccc2C)cc1N1CCN(C)CC1 10.1021/jm980532e
276 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
5312149 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
CHEMBL431298 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
44398570 135183 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 392 4 2 4 3.7 O=S(=O)(Oc1ccc2[nH]cc(C3CCNCC3)c2c1)c1c(F)cccc1F 10.1021/jm050247c
CHEMBL372006 135183 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 392 4 2 4 3.7 O=S(=O)(Oc1ccc2[nH]cc(C3CCNCC3)c2c1)c1c(F)cccc1F 10.1021/jm050247c
23625763 16674 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 367 3 1 6 3.1 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL1242614 16674 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 367 3 1 6 3.1 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
52946845 16682 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 407 3 1 8 2.8 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
CHEMBL1242702 16682 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 407 3 1 8 2.8 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
71459954 79182 0 None 9 7 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
CHEMBL2113386 79182 0 None 9 7 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
10136837 165963 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
CHEMBL425196 165963 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
10154392 133516 11 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
CHEMBL370779 133516 11 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
9891618 107124 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 107124 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 107408 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 107408 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
9890119 208057 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 208057 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
276 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
5312149 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
CHEMBL431298 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
6918689 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
CHEMBL23038 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
137646045 157789 0 None 436 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 404 4 0 5 4.3 CN(C)CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4083059 157789 0 None 436 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 404 4 0 5 4.3 CN(C)CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
16117151 60087 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 60087 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 60087 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117279 60136 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 60136 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 60136 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
4106 2502 22 None -2 34 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
5358812 2502 22 None -2 34 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
89 2502 22 None -2 34 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
CHEMBL93240 2502 22 None -2 34 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
10108884 181065 0 None 30 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4759730 181065 0 None 30 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
134147097 149827 0 None 251 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3cccc4ccccc34)c21 10.1016/j.bmc.2016.10.010
CHEMBL3948819 149827 0 None 251 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3cccc4ccccc34)c21 10.1016/j.bmc.2016.10.010
134156091 151393 0 None 794 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2cc3ccn(S(=O)(=O)c4cccc5ccccc45)c3cc21 10.1016/j.bmc.2016.10.010
CHEMBL3961596 151393 0 None 794 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2cc3ccn(S(=O)(=O)c4cccc5ccccc45)c3cc21 10.1016/j.bmc.2016.10.010
164619537 185555 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4863218 185555 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113783
162656068 180816 0 None 288 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756814 180816 0 None 288 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
126720397 181095 0 None 467 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760105 181095 0 None 467 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
162657540 181123 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 403 4 1 7 2.3 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760545 181123 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 403 4 1 7 2.3 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
46889349 7082 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085036 7082 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890266 7424 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 6 2 4 2.1 CNS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086573 7424 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 6 2 4 2.1 CNS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10115854 69599 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193450 69599 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10291754 70434 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL194590 70434 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
9842551 127223 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365774 127223 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10274389 133422 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370507 133422 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
9902533 133602 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133602 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10136837 165963 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL425196 165963 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44433193 88721 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236103 88721 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435625 148998 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL394233 148998 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44403297 133008 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL370209 133008 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
10201610 133577 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371176 133577 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10154392 133516 11 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.08.059
CHEMBL370779 133516 11 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.08.059
23655465 89388 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL236987 89388 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
11772625 82015 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepinDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepin
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165519 82015 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepinDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepin
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2C1 10.1016/j.bmcl.2012.06.002
276 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 3513 50 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
6918689 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL23038 85984 4 None 812 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1016/j.bmcl.2007.11.045
10407367 196793 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 196793 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
10449488 196866 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565976 196866 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836616 18803 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278179 18803 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
135804742 198035 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 5 5 4 2.2 C/C(=N\NC(=N)N)c1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm900796p
CHEMBL573982 198035 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 5 5 4 2.2 C/C(=N\NC(=N)N)c1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm900796p
136123549 198537 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 400 6 5 5 2.2 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(/C(C)=N/NC(=N)N)c3c2)cc1 10.1021/jm900796p
CHEMBL578023 198537 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 400 6 5 5 2.2 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(/C(C)=N/NC(=N)N)c3c2)cc1 10.1021/jm900796p
71151588 118258 0 None -10 10 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 118258 0 None -10 10 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
10162467 123666 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 4 2 4 6.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL362063 123666 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 4 2 4 6.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
10182228 132449 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 9 2 3 5.5 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
CHEMBL369759 132449 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 9 2 3 5.5 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
71459954 79182 0 None 9 7 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 79182 0 None 9 7 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
11314681 201729 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
CHEMBL606546 201729 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
11200511 201730 0 None 15 8 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 201730 0 None 15 8 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
11453792 201731 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606548 201731 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
11385064 201734 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606557 201734 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
11211722 201735 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606558 201735 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11246907 201749 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606636 201749 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11486933 201750 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606637 201750 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
11419238 201751 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606638 201751 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
11316095 201788 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606817 201788 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
11234629 202213 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL609741 202213 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
11749539 202241 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
CHEMBL609992 202241 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
11280663 202244 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
CHEMBL609995 202244 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
11260183 202245 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 481 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(I)cc1 10.1021/jm049243i
CHEMBL609996 202245 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 481 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(I)cc1 10.1021/jm049243i
11474995 202294 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 397 6 3 3 4.4 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
CHEMBL610253 202294 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 397 6 3 3 4.4 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
11451904 202295 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL610254 202295 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
68108804 131689 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131689 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
57414530 131706 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 0 4 3.9 CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692925 131706 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 0 4 3.9 CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
58258786 127925 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127925 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
58258778 127927 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127927 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
16118923 60146 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 60146 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 60146 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
118654365 191832 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5198847 191832 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
49836618 18643 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276838 18643 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
10430623 18675 24 None 213 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18675 24 None 213 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
68115674 131782 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3693001 131782 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
68115749 132269 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 132269 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
162674158 183003 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4793608 183003 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
150 2509 21 None -2 16 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2509 21 None -2 16 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2509 21 None -2 16 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2509 21 None -2 16 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2509 21 None -2 16 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
9948345 80058 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm5003952
CHEMBL212995 80058 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm5003952
118712407 114164 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 404 4 1 9 1.4 CSc1nn2c(N3CCNCC3)nc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL3329434 114164 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 404 4 1 9 1.4 CSc1nn2c(N3CCNCC3)nc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm5003952
11371056 114166 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 334 5 0 5 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2sccc12 10.1021/jm5003952
CHEMBL3329436 114166 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 334 5 0 5 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2sccc12 10.1021/jm5003952
11983287 114169 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 416 6 2 6 3.7 COc1ccc(C)cc1S(=O)(=O)Nc1cc(OC2CCNCC2)c2occc2c1 10.1021/jm5003952
CHEMBL3329439 114169 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 416 6 2 6 3.7 COc1ccc(C)cc1S(=O)(=O)Nc1cc(OC2CCNCC2)c2occc2c1 10.1021/jm5003952
57403057 70771 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70771 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
57394333 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127930 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127930 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258852 127953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5[nH]ccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664778 127953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5[nH]ccc45)ccc31)C1CCC(C2)N1 nan
58258767 128976 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 4 5.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1Cc1ccccc1 nan
CHEMBL3669653 128976 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 4 5.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1Cc1ccccc1 nan
58258875 128977 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1CCO nan
CHEMBL3669654 128977 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1CCO nan
58258807 128988 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1cn(S(=O)(=O)c2cc(OC)c3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3669665 128988 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1cn(S(=O)(=O)c2cc(OC)c3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258853 128998 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669675 128998 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
1346 83 117 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
280 83 117 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
9899402 83 117 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
CHEMBL9666 83 117 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
42631003 199618 13 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
CHEMBL592752 199618 13 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
42631003 199618 13 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
CHEMBL592752 199618 13 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
9948345 80058 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm060469q
CHEMBL212995 80058 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm060469q
44435650 88510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235118 88510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57403057 70771 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70771 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57394333 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263299 192118 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520343 192118 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
44474629 14079 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL1197581 14079 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL577570 14079 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
57414656 131707 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 3 0 4 4.3 CCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692926 131707 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 3 0 4 4.3 CCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
57414660 131713 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692932 131713 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
68115810 131736 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 419 4 1 5 4.0 CC(C)(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692955 131736 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 419 4 1 5 4.0 CC(C)(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
68115719 131763 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692982 131763 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
68115680 132237 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.5 Cc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696950 132237 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.5 Cc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
44435650 88510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235118 88510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
17940113 47118 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 6 2.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL154273 47118 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 6 2.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
18354589 47230 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2cccc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154367 47230 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2cccc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940199 50282 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 421 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157173 50282 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 421 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940155 119869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 381 5 2 5 2.6 COc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL348870 119869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 381 5 2 5 2.6 COc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918578 207676 1 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 430 4 2 5 3.7 Cc1cc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)c(C)cc1Cl 10.1016/s0960-894x(01)00558-3
CHEMBL95388 207676 1 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 430 4 2 5 3.7 Cc1cc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)c(C)cc1Cl 10.1016/s0960-894x(01)00558-3
9805456 207746 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 207746 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891617 207982 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
CHEMBL97211 207982 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
9870053 208284 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 208284 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
10528182 202640 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2c(C)sc3ccc(Cl)cc23)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL61318 202640 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2c(C)sc3ccc(Cl)cc23)cc1N1CCN(C)CC1 10.1021/jm980532e
136046098 67359 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 2 5 3.4 COc1cccc(-c2noc(-c3[nH]c4ccccc4c3CCN)n2)c1 10.1021/jm050247c
CHEMBL188600 67359 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 2 5 3.4 COc1cccc(-c2noc(-c3[nH]c4ccccc4c3CCN)n2)c1 10.1021/jm050247c
9867263 162432 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1021/jm050247c
CHEMBL416638 162432 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1021/jm050247c
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
9805456 207746 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 207746 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891617 207982 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
CHEMBL97211 207982 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
9870053 208284 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 208284 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
46889329 7348 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 1 4 2.5 CN(CC(N)=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086253 7348 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 1 4 2.5 CN(CC(N)=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889352 7391 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 441 8 2 5 2.9 O=S(=O)(O)CCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086476 7391 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 441 8 2 5 2.9 O=S(=O)(O)CCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
10156556 72029 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 5 2.7 O=S(=O)(c1ccccc1)c1coc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL197574 72029 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 5 2.7 O=S(=O)(c1ccccc1)c1coc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
11689373 93467 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246078 93467 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44441237 93671 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 392 3 2 6 1.4 Nc1ccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cc(F)cc32)cc1 10.1016/j.bmcl.2006.12.093
CHEMBL246917 93671 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 392 3 2 6 1.4 Nc1ccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cc(F)cc32)cc1 10.1016/j.bmcl.2006.12.093
44425701 86305 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 372 6 1 3 3.9 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL231334 86305 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 372 6 1 3 3.9 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
44435610 88795 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236404 88795 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435629 148694 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL393997 148694 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435613 154403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL398809 154403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
16071605 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
7356 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
CHEMBL2103880 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
DB12229 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
16071605 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
7356 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
CHEMBL2103880 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
DB12229 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
57394333 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258790 128987 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 3 1 7 3.1 COc1cc(S(=O)(=O)n2ncc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669664 128987 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 3 1 7 3.1 COc1cc(S(=O)(=O)n2ncc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258821 129010 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669687 129010 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
10047631 204871 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL75734 204871 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)c1 10.1016/s0960-894x(00)00453-4
135437144 112337 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm010943m
CHEMBL329329 112337 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm010943m
16071605 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
7356 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
CHEMBL2103880 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
DB12229 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
135437144 112337 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm030030n
CHEMBL329329 112337 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm030030n
4106 2502 22 None -2 34 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
5358812 2502 22 None -2 34 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
89 2502 22 None -2 34 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
CHEMBL93240 2502 22 None -2 34 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmc.2023.117256
118181459 190041 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 389 4 1 6 2.4 COc1ccc(S(=O)(=O)n2ccc3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5171917 190041 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 389 4 1 6 2.4 COc1ccc(S(=O)(=O)n2ccc3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
168280735 191070 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 451 5 2 6 4.1 COc1cc(NS(=O)(=O)c2sc3cc(Cl)ccc3c2C)ccc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5187416 191070 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 451 5 2 6 4.1 COc1cc(NS(=O)(=O)c2sc3cc(Cl)ccc3c2C)ccc1N1CCNCC1 10.1016/j.bmc.2022.116917
118879893 161203 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4080401 161203 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117763 161203 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
44435610 88795 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236404 88795 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435629 148694 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393997 148694 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435613 154403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398809 154403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880708 7446 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1086719 7446 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
57394333 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70772 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
9867263 162432 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL416638 162432 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
25263302 191984 0 None 134 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191984 0 None 134 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
25263303 184184 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 282 4 1 3 3.0 Cc1c(OCc2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483148 184184 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 282 4 1 3 3.0 Cc1c(OCc2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
68115638 131698 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692917 131698 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
68115676 132236 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696949 132236 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
44388701 123135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL361213 123135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
52913108 70761 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70761 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
58258809 127916 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664740 127916 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127930 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127930 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258812 128975 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 5 4.2 COCCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669652 128975 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 5 4.2 COCCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258818 128986 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 488 6 1 6 4.9 COc1cc(S(=O)(=O)c2cccc(OCc3ccccc3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669663 128986 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 488 6 1 6 4.9 COc1cc(S(=O)(=O)c2cccc(OCc3ccccc3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44388701 123135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1016/j.bmcl.2012.06.002
CHEMBL361213 123135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1016/j.bmcl.2012.06.002
9863836 207624 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1021/jm030030n
CHEMBL95136 207624 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1021/jm030030n
53318109 60103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642849 60103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739254 60103 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
11256720 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
9444 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
CHEMBL1083390 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
DB12680 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
3052776 206556 90 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1016/j.ejmech.2020.112765
CHEMBL887 206556 90 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1016/j.ejmech.2020.112765
11256720 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
11256720 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
9444 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL1083390 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
DB12680 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
44433195 146885 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392541 146885 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435616 147854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393312 147854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11256720 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
9444 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
CHEMBL1083390 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
DB12680 2055 79 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
164619210 185663 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4864854 185663 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
9863836 207624 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL95136 207624 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.045
49836923 18763 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277918 18763 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
52945634 16689 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 4 0 8 3.5 CCN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242791 16689 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 4 0 8 3.5 CCN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435616 147854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393312 147854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258786 127925 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127925 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
24965679 84035 19 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207386 84035 19 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
10531 1420 21 None -9 23 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1420 21 None -9 23 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1420 21 None -9 23 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1420 21 None -9 23 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1420 21 None -9 23 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
9862256 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL92139 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258758 128966 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128966 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
58258757 128996 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669673 128996 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258838 129016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669693 129016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
9862256 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
9822215 207110 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
CHEMBL92093 207110 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
9862256 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL92139 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44438738 148562 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 368 4 0 4 3.9 CN(C)CC1CCCc2c1c1ccccc1n2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.12.089
CHEMBL393886 148562 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 368 4 0 4 3.9 CN(C)CC1CCCc2c1c1ccccc1n2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.12.089
16117280 60137 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642887 60137 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739614 60137 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16071847 60145 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 60145 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 60145 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44216882 139115 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786752 139115 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
44403094 135225 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 344 5 0 5 2.9 COc1ccc2c(c1)c(CN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
CHEMBL372364 135225 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 344 5 0 5 2.9 COc1ccc2c(c1)c(CN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
44435619 88783 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236335 88783 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435608 89140 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236577 89140 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880758 6095 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080729 6095 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
52913108 70761 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70761 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263354 192317 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2cccc3ccccc23)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL520638 192317 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2cccc3ccccc23)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
9862256 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL92139 207120 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
68109269 131635 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 2 1 5 3.4 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccc(F)cc21 nan
CHEMBL3692855 131635 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 2 1 5 3.4 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccc(F)cc21 nan
68115826 131748 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 4 2 6 2.4 COc1cc(S(=O)(=O)c2ccccc2CO)cc2c3c(oc12)CCNC3 nan
CHEMBL3692967 131748 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 4 2 6 2.4 COc1cc(S(=O)(=O)c2ccccc2CO)cc2c3c(oc12)CCNC3 nan
68115682 132242 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696955 132242 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
1042 1581 23 None -5 17 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1581 23 None -5 17 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1581 23 None -5 17 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1581 23 None -5 17 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1581 23 None -5 17 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
44435619 88783 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236335 88783 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435608 89140 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236577 89140 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
17940260 48112 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2ccccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155106 48112 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2ccccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940058 50474 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 447 6 1 7 1.9 COc1ccc(S(=O)(=O)N2CCc3c(OC)ccc(OC)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157338 50474 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 447 6 1 7 1.9 COc1ccc(S(=O)(=O)N2CCc3c(OC)ccc(OC)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918579 207756 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 494 4 2 5 3.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(I)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL95878 207756 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 494 4 2 5 3.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(I)cc1 10.1016/s0960-894x(01)00558-3
9935750 208447 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 5 2 6 5.4 CC(C)c1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL99982 208447 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 5 2 6 5.4 CC(C)c1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
134137966 147422 0 None 794 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 326 4 1 4 2.7 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c21 10.1016/j.bmc.2016.10.010
CHEMBL3929918 147422 0 None 794 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 326 4 1 4 2.7 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c21 10.1016/j.bmc.2016.10.010
46890189 7047 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 4 1 4 3.4 COC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084874 7047 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 4 1 4 3.4 COC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890191 7048 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 0 3 3.6 CC(=O)N(C)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084875 7048 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 0 3 3.6 CC(=O)N(C)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10177503 69820 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193665 69820 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
18180095 114420 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 477 4 1 6 4.4 Cc1c(S(=O)(=O)Nc2cc3c(c(N4CCN(C)CC4)c2)OCC3)sc2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL3331585 114420 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 477 4 1 6 4.4 Cc1c(S(=O)(=O)Nc2cc3c(c(N4CCN(C)CC4)c2)OCC3)sc2ccc(Cl)cc12 10.1021/jm5003952
58258764 127939 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127939 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258761 128999 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669676 128999 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258822 129002 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669679 129002 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
9953284 204796 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.05.076
CHEMBL75010 204796 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.05.076
9953284 204796 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00453-4
CHEMBL75010 204796 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00453-4
71458811 82016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165520 82016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
118654427 192379 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5207516 192379 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
57396970 69743 0 None 4 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69743 0 None 4 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
11461668 62557 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 330 6 1 5 2.5 CNCCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL178254 62557 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 330 6 1 5 2.5 CNCCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.113792
71458811 82016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
CHEMBL2165520 82016 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
11725505 199039 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585930 199039 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
9978683 18674 0 None 208 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18674 0 None 208 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
44554395 18723 0 None 54 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18723 0 None 54 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
23725134 14054 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL1197475 14054 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL573521 14054 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
66801234 112101 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289995 112101 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68109281 131677 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CO)NCC3 nan
CHEMBL3692896 131677 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CO)NCC3 nan
57414792 131735 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.3 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCO)CC3 nan
CHEMBL3692954 131735 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.3 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCO)CC3 nan
68115811 131738 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 5 0 5 3.9 COCCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692957 131738 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 5 0 5 3.9 COCCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
68115846 132255 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 5 2 6 2.3 O=S(=O)(c1ccccc1)c1cc(OCCO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696968 132255 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 5 2 6 2.3 O=S(=O)(c1ccccc1)c1cc(OCCO)c2oc3c(c2c1)CNCC3 nan
10388593 161033 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4100484 161033 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116439 161033 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
52940867 16675 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 463 4 0 8 4.3 CC(C)N1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242615 16675 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 463 4 0 8 4.3 CC(C)N1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
11961315 114155 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2c1CC[C@H](N(C)C)C2 10.1021/jm5003952
CHEMBL3329425 114155 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2c1CC[C@H](N(C)C)C2 10.1021/jm5003952
58258797 129005 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669682 129005 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44397689 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL196102 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL373107 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
16019576 10897 6 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10897 6 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
16118797 60097 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642852 60097 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739216 60097 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
164613488 185020 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4854972 185020 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113783
137633076 156549 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 7 0 6 4.1 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068232 156549 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 7 0 6 4.1 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
44433199 88776 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236314 88776 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
276 3513 50 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
5312149 3513 50 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
CHEMBL431298 3513 50 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
9933223 101539 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL298274 101539 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
44397689 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL196102 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL373107 71440 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
45487139 197340 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL568935 197340 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
49836825 18722 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
CHEMBL1277564 18722 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
49836826 18732 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277656 18732 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836509 18771 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277999 18771 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
71502633 118260 0 None 64 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 533 10 0 7 5.3 CC(C)Oc1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409258 118260 0 None 64 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 533 10 0 7 5.3 CC(C)Oc1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
68109203 131655 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3692874 131655 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CCNC3 nan
68108804 131689 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131689 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
68115644 131740 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692959 131740 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
162654074 180579 0 None -3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4754138 180579 0 None -3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
12148615 114177 0 None - 1 Human 8.7 pKi = 8.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 344 4 1 4 4.1 NCCOc1cccc2c1c1cccc3c1n2[C@H](c1ccccc1)CO3 10.1021/jm5003952
CHEMBL3329447 114177 0 None - 1 Human 8.7 pKi = 8.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 344 4 1 4 4.1 NCCOc1cccc2c1c1cccc3c1n2[C@H](c1ccccc1)CO3 10.1021/jm5003952
52913104 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258764 127939 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127939 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258758 128966 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128966 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
58258761 128999 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669676 128999 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258769 129001 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 129001 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
44413495 77998 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
CHEMBL209724 77998 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
58158721 138992 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785453 138992 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
52913104 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
24776942 166695 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@H]1CCCN1C 10.1021/jm070910s
CHEMBL428238 166695 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@H]1CCCN1C 10.1021/jm070910s
49836827 18741 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277751 18741 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836828 18749 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277836 18749 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
25263300 184618 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484926 184618 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
66801210 112124 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
CHEMBL3290017 112124 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
16222549 82020 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165524 82020 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
52913104 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258786 127925 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127925 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
58258794 128960 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669637 128960 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
58258754 128969 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128969 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
44438722 93822 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 0 4 4.0 CN(C)CCc1cn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247673 93822 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 0 4 4.0 CN(C)CCc1cn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
44435652 89254 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236812 89254 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
52913104 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70759 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44405357 135491 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 3 6 2.5 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL372853 135491 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 3 6 2.5 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
44554394 18733 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277657 18733 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
10383646 18762 0 None 186 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18762 0 None 186 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
142592130 173348 0 None 263 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4527051 173348 0 None 263 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
11154465 60564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
CHEMBL175940 60564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
68109036 131642 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1ccc(Cl)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692862 131642 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1ccc(Cl)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116256 131753 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692972 131753 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115706 131760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692979 131760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
68115844 132251 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696964 132251 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115747 132268 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 3 1 4 4.2 COc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696981 132268 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 3 1 4 4.2 COc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
44435652 89254 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236812 89254 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
16222547 82038 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165541 82038 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
44369594 49064 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 6 2 6 2.9 COc1cc(Cl)c(C)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL156130 49064 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 6 2 6 2.9 COc1cc(Cl)c(C)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
17940245 50224 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2ccc(I)cc2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157103 50224 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2ccc(I)cc2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10433930 51089 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157910 51089 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9957092 107212 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316643 107212 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
17940089 119663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346990 119663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328732 207594 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 512 4 1 6 5.5 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN5CCC[C@H]5C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL94988 207594 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 512 4 1 6 5.5 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN5CCC[C@H]5C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918577 207702 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2c(Cl)cc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL95568 207702 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2c(Cl)cc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
6918603 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9847669 208181 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2c(Cl)cccc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL98353 208181 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2c(Cl)cccc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
10526615 102506 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 429 5 1 5 3.6 COc1ccc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL304039 102506 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 429 5 1 5 3.6 COc1ccc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
11154465 60564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm050247c
CHEMBL175940 60564 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm050247c
6918603 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL97158 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
10320800 16667 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 3 0 8 3.5 CN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242517 16667 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 3 0 8 3.5 CN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435603 91750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL240922 91750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435640 154929 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL401019 154929 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
6918603 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 207971 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
46890267 6605 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 426 6 1 4 2.5 CN(C)S(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083173 6605 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 426 6 1 4 2.5 CN(C)S(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890220 6754 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 405 5 2 4 3.0 CC(C)(O)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083780 6754 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 405 5 2 4 3.0 CC(C)(O)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889920 7202 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 291 3 2 4 1.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cn[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085619 7202 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 291 3 2 4 1.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cn[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
10273087 134802 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371876 134802 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
22557214 93468 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1cccc(Cl)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246079 93468 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1cccc(Cl)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
20765662 93575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 398 3 1 6 1.9 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1C#N)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246500 93575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 398 3 1 6 1.9 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1C#N)CCO2 10.1016/j.bmcl.2006.12.093
42631003 199618 13 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 199618 13 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
9863611 96930 0 None 7 5 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 358 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCNCC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL266018 96930 0 None 7 5 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 358 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCNCC3)cc1 10.1016/j.bmcl.2006.10.036
118712402 114156 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 306 3 1 2 4.2 Fc1ccc2c(c1)c(C1=CCNCC1)cn2Cc1ccccc1 10.1021/jm5003952
CHEMBL3329426 114156 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 306 3 1 2 4.2 Fc1ccc2c(c1)c(C1=CCNCC1)cn2Cc1ccccc1 10.1021/jm5003952
135847967 114184 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 337 3 3 4 3.4 Clc1ccc(-c2[nH]c3ccccc3c2/C=N/NC2=NCCN2)cc1 10.1021/jm5003952
CHEMBL3329454 114184 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 337 3 3 4 3.4 Clc1ccc(-c2[nH]c3ccccc3c2/C=N/NC2=NCCN2)cc1 10.1021/jm5003952
58258840 127920 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)cc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664744 127920 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)cc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258838 129016 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669693 129016 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44389002 63564 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180066 63564 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44389001 63801 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180221 63801 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
563919 99278 5 None 1000 2 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL281937 99278 5 None 1000 2 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
10498813 201760 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 361 5 1 5 2.2 COc1ccc(NS(=O)(=O)c2ccccc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL60669 201760 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 361 5 1 5 2.2 COc1ccc(NS(=O)(=O)c2ccccc2)cc1N1CCN(C)CC1 10.1021/jm980532e
44263491 135197 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmc.2009.08.006
CHEMBL372109 135197 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmc.2009.08.006
16718920 189677 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL515307 189677 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
46227404 199883 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL594548 199883 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
135398745 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
135398745 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2914 112 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
135398737 958 93 None -4 89 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
38 958 93 None -4 89 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
722 958 93 None -4 89 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
CHEMBL42 958 93 None -4 89 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
DB00363 958 93 None -4 89 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
31101 729 40 None -23 36 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 729 40 None -23 36 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 729 40 None -23 36 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 729 40 None -23 36 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 729 40 None -23 36 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
56945043 156405 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4066532 156405 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
56944956 158919 0 None -10 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4095555 158919 0 None -10 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
134155367 151215 0 None 125 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3959964 151215 0 None 125 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
90469382 186163 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4872451 186163 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.1c00224
164612723 184687 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 554 11 2 7 5.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850051 184687 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 554 11 2 7 5.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
162655699 180804 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 373 4 1 8 1.1 COc1cccc(S(=O)(=O)n2cnc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756605 180804 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 373 4 1 8 1.1 COc1cccc(S(=O)(=O)n2cnc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
134130058 142242 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 11 0 6 5.3 CN(CCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3884709 142242 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 11 0 6 5.3 CN(CCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
134130237 142259 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 9 0 6 4.5 CN(CCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3884867 142259 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 9 0 6 4.5 CN(CCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
134130116 142272 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 565 7 1 7 5.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884988 142272 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 565 7 1 7 5.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
53310757 139134 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786973 139134 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
9969402 70547 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194750 70547 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
10272846 71785 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 1 4 4.4 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196743 71785 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 1 4 4.4 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44263491 135197 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL372109 135197 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmcl.2005.08.059
16718920 189677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
CHEMBL515307 189677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
155528355 171335 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 424 5 2 6 3.5 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4461327 171335 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 424 5 2 6 3.5 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155533660 171901 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4469792 171901 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
155538873 172789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4513458 172789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155514576 176550 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4441060 176550 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4597227 176550 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
155515920 176684 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4442332 176684 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4598348 176684 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
23655462 90223 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL238277 90223 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
44435538 90606 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
CHEMBL238770 90606 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
21071574 124083 1 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL363275 124083 1 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
90656165 110836 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 386 3 1 4 3.6 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260798 110836 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 386 3 1 4 3.6 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
90656170 110841 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2cccc(Cl)c2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260803 110841 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2cccc(Cl)c2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
22557257 93469 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1cccc(F)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246080 93469 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1cccc(F)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44425705 86080 0 None 1 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 411 4 1 5 3.8 Cc1noc(C)c1-c1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL230930 86080 0 None 1 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 411 4 1 5 3.8 Cc1noc(C)c1-c1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
10217687 86231 0 None -12 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 456 5 1 4 4.8 COc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231249 86231 0 None -12 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 456 5 1 4 4.8 COc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
11235953 201786 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606815 201786 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
68109159 131685 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131685 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414662 131716 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 1 5 4.0 O=S(=O)(c1ccc(C2CCO2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692935 131716 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 1 5 4.0 O=S(=O)(c1ccc(C2CCO2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25263350 184371 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccccc1S(=O)(=O)Oc1cccc(C2CCNCC2)c1C 10.1016/j.bmcl.2009.03.077
CHEMBL484533 184371 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccccc1S(=O)(=O)Oc1cccc(C2CCNCC2)c1C 10.1016/j.bmcl.2009.03.077
11744377 157062 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4074058 157062 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
23652788 56692 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 511 3 0 5 4.2 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642423 56692 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 511 3 0 5 4.2 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
21071574 124083 1 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
CHEMBL363275 124083 1 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
10390318 156263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(Br)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4064995 156263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(Br)cc1 10.1021/acs.jmedchem.6b01662
24768515 127507 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/jm070521y
CHEMBL366151 127507 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/jm070521y
25263304 184185 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2cccc(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483149 184185 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2cccc(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
71449796 82048 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2F)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165551 82048 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2F)C1 10.1016/j.bmcl.2012.06.002
44403072 70409 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194568 70409 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
25263336 184335 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484337 184335 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
23652790 56689 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 465 4 0 5 3.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642420 56689 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 465 4 0 5 3.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
135398745 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
47 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
DB00334 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
135398745 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
47 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
DB00334 2914 112 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
46880529 6171 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
CHEMBL1081110 6171 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
23653062 56693 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642424 56693 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
24775948 84470 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2220110 84470 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL3216123 84470 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
23652557 56683 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 389 3 0 5 3.3 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642414 56683 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 389 3 0 5 3.3 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
44435622 89100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236540 89100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162661196 181461 0 None -14 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4764468 181461 0 None -14 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
58258826 127958 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4O)ccc31)C1CCC(C2)N1 nan
CHEMBL3664783 127958 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4O)ccc31)C1CCC(C2)N1 nan
1342 35 49 None -45 19 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
3 35 49 None -45 19 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
CHEMBL277120 35 49 None -45 19 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
5 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
5202 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
CHEMBL39 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
DB08839 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
44401278 71088 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 277 6 1 1 4.4 CNCCC1=CC(CCc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL195317 71088 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 277 6 1 1 4.4 CNCCC1=CC(CCc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
5 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
5202 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
CHEMBL39 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
DB08839 139 72 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
135398737 958 93 None -4 89 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 958 93 None -4 89 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 958 93 None -4 89 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 958 93 None -4 89 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 958 93 None -4 89 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
4106 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
56944861 157074 0 None -38 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4074195 157074 0 None -38 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
66801430 157714 0 None -1 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 7 2 3 4.9 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4081987 157714 0 None -1 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 7 2 3 4.9 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
137642284 158220 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4088170 158220 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
162672328 182993 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 538 9 1 5 5.8 C#CCNC1CCc2c(OCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4793457 182993 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 538 9 1 5 5.8 C#CCNC1CCc2c(OCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
137654042 158839 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(Cl)cccc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4094743 158839 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(Cl)cccc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
4106 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2502 22 None -7 34 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
71463515 85295 3 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 1 2 1.7 CN(C)CCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260373 85295 3 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 1 2 1.7 CN(C)CCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
118732439 118388 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 427 6 1 6 3.6 CN(C)CCn1c(=O)sc2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc21 10.1016/j.ejmech.2015.01.052
CHEMBL3410504 118388 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 427 6 1 6 3.6 CN(C)CCn1c(=O)sc2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc21 10.1016/j.ejmech.2015.01.052
155532983 171813 0 None 51 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 369 3 1 6 3.9 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4468396 171813 0 None 51 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 369 3 1 6 3.9 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
90656154 110825 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 340 2 1 2 3.5 O=C1CC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260786 110825 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 340 2 1 2 3.5 O=C1CC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
71152026 118243 0 None -8 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccc(F)cc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409241 118243 0 None -8 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccc(F)cc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
56944565 112049 0 None -251 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289944 112049 0 None -251 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
56945046 112060 0 None -16 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 7 1 6 4.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289955 112060 0 None -16 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 7 1 6 4.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
66801186 112125 0 None -30 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 457 7 1 7 3.2 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3290018 112125 0 None -30 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 457 7 1 7 3.2 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
66801246 112126 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 471 8 1 7 3.6 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3290019 112126 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 471 8 1 7 3.6 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
68115610 131626 0 None - 1 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccc(CO)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692846 131626 0 None - 1 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccc(CO)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
11166043 61388 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL177005 61388 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
1809 134 32 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
4 134 32 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
CHEMBL18840 134 32 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
11408954 157416 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 477 7 1 7 4.7 O=S(=O)(Nc1ccc2c(ccn2CCCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
CHEMBL407860 157416 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 477 7 1 7 4.7 O=S(=O)(Nc1ccc2c(ccn2CCCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
10708918 208097 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm050247c
CHEMBL97819 208097 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm050247c
CHEMBL5074190 214314 0 None -398 9 Human 6.0 pKi = 6 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
10708918 208097 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm030030n
CHEMBL97819 208097 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm030030n
33630 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178957 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
124087 1389 114 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1389 114 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1389 114 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1389 114 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1389 114 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
164628882 186450 0 None -5011 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 477 6 0 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3C(=O)c4ccccc4S3(=O)=O)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4876545 186450 0 None -5011 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 477 6 0 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3C(=O)c4ccccc4S3(=O)=O)cc2)CC1 10.1016/j.bmcl.2021.128028
155519393 170419 0 None 8 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 397 7 2 4 5.3 COc1ccc2[nH]cc(CCNCc3ccc(-c4cnc5ccccc5c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4448285 170419 0 None 8 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 397 7 2 4 5.3 COc1ccc2[nH]cc(CCNCc3ccc(-c4cnc5ccccc5c4)o3)c2c1 10.1016/j.ejmech.2019.111857
164619290 185805 0 None -6 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 463 7 0 5 4.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4866981 185805 0 None -6 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 463 7 0 5 4.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2021.128028
126720429 162950 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4174680 162950 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
57390799 70769 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 356 2 1 6 2.1 Cn1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)n1 10.1016/j.bmcl.2012.01.022
CHEMBL1950771 70769 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 356 2 1 6 2.1 Cn1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)n1 10.1016/j.bmcl.2012.01.022
44395458 125041 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 6 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL364351 125041 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 6 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
11522698 94109 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 325 6 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL249188 94109 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 325 6 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
137660741 159369 0 None -33 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4100470 159369 0 None -33 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL5283896 194234 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 643 11 0 8 5.8 O=C1CC2CCc3ccsc3C2=NN1CCCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
71462179 81429 0 None -7 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 406 7 1 5 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159472 81429 0 None -7 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 406 7 1 5 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
71455002 81446 0 None -51 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159489 81446 0 None -51 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
155544836 175018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4567160 175018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
156019563 177987 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 364 5 0 4 4.1 C=CCOc1c(OC)cc2c3c1-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4646172 177987 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 364 5 0 4 4.1 C=CCOc1c(OC)cc2c3c1-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL5073337 214292 0 None -24 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccc(Cl)cc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
137645926 157565 0 None -27 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4080398 157565 0 None -27 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
3191 102858 97 None -15 25 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 97 None -15 25 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44456033 155567 3 None -794 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155567 3 None -794 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
49799703 10992 4 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173577 10992 4 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
9903598 204363 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 272 4 0 3 3.1 COc1ccc2c(c1)c(CCN(C)C)c1n2CCCC1 10.1021/jm990550b
CHEMBL7172 204363 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 272 4 0 3 3.1 COc1ccc2c(c1)c(CCN(C)C)c1n2CCCC1 10.1021/jm990550b
155524491 170956 0 None -128 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccccc2Cl)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4455658 170956 0 None -128 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccccc2Cl)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155534184 171942 0 None -67 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccccc2F)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4470437 171942 0 None -67 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccccc2F)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155514505 169848 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 1 4 5.2 COc1cccc(-c2ccc(CNC(C)Cc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4440075 169848 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 1 4 5.2 COc1cccc(-c2ccc(CNC(C)Cc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155553745 175445 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4576700 175445 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
13069622 120616 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360999 120616 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546120 120616 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
134147124 149980 0 None -19 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2ncccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3950020 149980 0 None -19 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2ncccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
58258824 127951 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)ccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664776 127951 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)ccn4)ccc31)C1CCC(C2)N1 nan
1342 35 49 None -45 19 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 35 49 None -45 19 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 35 49 None -45 19 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
145986138 165469 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239705 165469 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
137644790 158068 0 None -28 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4086211 158068 0 None -28 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
1016 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
2561 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
2733526 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
5384 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
CHEMBL83 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
DB00675 3747 78 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
3158 56267 27 None -851 20 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011657
CHEMBL1628227 56267 27 None -851 20 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011657
155532396 171795 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 399 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4468014 171795 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 399 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
57399866 71541 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949974 71541 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1962960 71541 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
44420568 166205 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 1 2 3.9 COc1ccc2[nH]cc(CCN(C)Cc3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
CHEMBL426567 166205 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 1 2 3.9 COc1ccc2[nH]cc(CCN(C)Cc3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
68115788 132264 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 380 3 1 7 2.5 O=S(=O)(c1ccccc1)c1cc(-n2cncn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696977 132264 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 380 3 1 7 2.5 O=S(=O)(c1ccccc1)c1cc(-n2cncn2)c2oc3c(c2c1)CNCC3 nan
164618482 185915 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4868911 185915 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
53323441 60143 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642879 60143 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739647 60143 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
126720442 163039 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(Cl)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176014 163039 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(Cl)cc1 10.1016/j.ejmech.2017.12.053
155548275 173789 0 None 74 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 426 5 2 5 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4537701 173789 0 None 74 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 426 5 2 5 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
11408932 60993 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 476 3 0 5 5.2 Cc1c(S(=O)(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL176258 60993 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 476 3 0 5 5.2 Cc1c(S(=O)(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)sc2ccc(Cl)cc12 10.1021/jm049615n
134137332 143008 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2ncccc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3894679 143008 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2ncccc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
164621422 185776 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 465 8 1 5 4.9 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4866550 185776 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 465 8 1 5 4.9 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
86288948 112626 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233679 112626 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302600 112626 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
13437718 180498 10 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 273 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2c(O)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4753238 180498 10 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 273 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2c(O)cccc21 10.1016/j.ejmech.2020.112916
126720395 162550 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4168165 162550 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
11601955 94285 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 306 4 1 4 2.9 CN1CCN(c2ccc(C#N)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250401 94285 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 306 4 1 4 2.9 CN1CCN(c2ccc(C#N)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
11420098 60803 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 1 5 5.7 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL176162 60803 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 1 5 5.7 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
57400828 68428 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917349 68428 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
1353 1911 93 None -1047 83 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
3559 1911 93 None -1047 83 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
86 1911 93 None -1047 83 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL54 1911 93 None -1047 83 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
DB00502 1911 93 None -1047 83 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
168288545 191763 0 None -239 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 372 8 3 9 1.1 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5197737 191763 0 None -239 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 372 8 3 9 1.1 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
142601328 185003 0 None -69 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 185003 0 None -69 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209858 184554 1 None -6 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 184554 1 None -6 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
168289915 191554 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194614 191554 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155511424 169545 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 7 2 3 4.8 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccccc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4435529 169545 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 7 2 3 4.8 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccccc4)o3)c12 10.1016/j.ejmech.2019.111857
135367405 164196 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 164196 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4534980 213987 20 None 2 3 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000345a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000345a HTR6
ChEMBL None None None CN(C)[C@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1 10.6019/CHEMBL5212743
118712406 114163 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 3.1 Cc1cc(C)cc(S(=O)(=O)c2ccc3ccnc(N4CCNCC4)c3c2)c1 10.1021/jm5003952
CHEMBL3329433 114163 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 3.1 Cc1cc(C)cc(S(=O)(=O)c2ccc3ccnc(N4CCNCC4)c3c2)c1 10.1021/jm5003952
52913224 70764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950765 70764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 nan
52912983 127904 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc(O)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664729 127904 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc(O)cc4)ccc31)C1CCC(C2)N1 nan
67085672 127914 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 2 5 4.2 CC(C)Nc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664738 127914 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 2 5 4.2 CC(C)Nc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258860 127918 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1ccccc1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
CHEMBL3664742 127918 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1ccccc1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
58258829 128972 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669649 128972 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
9821904 19451 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1Cl 10.1021/jm010943m
CHEMBL129614 19451 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1Cl 10.1021/jm010943m
135398737 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
155523355 170748 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc2ncccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4452416 170748 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc2ncccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
155557772 174681 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4559172 174681 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
118626142 165820 0 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248491 165820 0 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
155542321 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
CHEMBL4520796 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
163196460 192691 3 None 3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 394 4 1 7 3.4 CN1CCN(c2nc(N)nc(C(C)(C)Sc3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2022.114645
CHEMBL5219240 192691 3 None 3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 394 4 1 7 3.4 CN1CCN(c2nc(N)nc(C(C)(C)Sc3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2022.114645
155542321 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4520796 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
118654519 191265 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5190429 191265 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
90469046 184654 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 392 3 1 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4849693 184654 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 392 3 1 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164610452 184498 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4847373 184498 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
155542321 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constant
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.bmcl.2021.128275
CHEMBL4520796 173125 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constant
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.bmcl.2021.128275
44403048 132705 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL369910 132705 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
44435622 89100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236540 89100 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
164628531 186464 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4876727 186464 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
52913224 70764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950765 70764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164609111 184387 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4845762 184387 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
164609145 184471 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4846931 184471 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
25024332 62950 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785055 62950 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C)cc3)c2)CC1 10.1021/ml100101u
44420491 83763 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c1c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.08.068
CHEMBL220566 83763 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c1c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.08.068
23655287 88688 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
CHEMBL235985 88688 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
127047898 139823 0 None 56 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 440 6 0 6 3.9 CCc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
CHEMBL3798953 139823 0 None 56 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 440 6 0 6 3.9 CCc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
49836717 18681 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277192 18681 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
71151756 118261 0 None 10 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 547 11 0 7 5.6 CC(C)Oc1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409259 118261 0 None 10 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 547 11 0 7 5.6 CC(C)Oc1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
57391618 71469 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71469 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71469 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57391567 71537 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71537 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71537 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57393363 71564 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71564 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71564 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
11441064 201778 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606764 201778 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
68115755 132263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1cc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)cn1 nan
CHEMBL3696976 132263 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1cc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)cn1 nan
58149664 127423 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
CHEMBL3659970 127423 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
44435633 89541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237389 89541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24965678 84021 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207372 84021 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44435633 89541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237389 89541 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
25024528 62958 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 4 0 5 4.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cc(C(F)(F)F)ccc3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1785062 62958 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 4 0 5 4.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cc(C(F)(F)F)ccc3Cl)c2)CC1 10.1021/ml100101u
45487128 197787 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571878 197787 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
25263353 184132 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 359 5 1 4 3.8 CCc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL482749 184132 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 359 5 1 4 3.8 CCc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
131999484 182603 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182603 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182603 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
44435631 89677 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237594 89677 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
137649408 157518 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4079859 157518 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44435631 89677 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237594 89677 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
137630144 161051 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4085003 161051 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116567 161051 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44240860 139182 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787525 139182 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
25263307 184238 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2ccccc2F)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483559 184238 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2ccccc2F)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
45484298 197297 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568673 197297 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
134131322 142208 0 None -1174 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(Cl)ccc1Cl 10.1016/j.ejmech.2016.09.008
CHEMBL3884161 142208 0 None -1174 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(Cl)ccc1Cl 10.1016/j.ejmech.2016.09.008
162663078 181994 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4780470 181994 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
23624297 56682 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642413 56682 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
56944863 156719 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4070254 156719 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
156020908 178031 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4646868 178031 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
145959871 162009 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)ccnc32)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4159555 162009 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)ccnc32)cc1 10.1016/j.ejmech.2017.12.053
54582158 62534 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782359 62534 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
54586019 62536 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782361 62536 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
49836718 18682 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277193 18682 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
66801115 112064 0 None -11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 506 7 1 7 4.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289959 112064 0 None -11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 506 7 1 7 4.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68108771 131681 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1CNCc2c1oc1c(Cl)cc(S(=O)(=O)c3ccccc3)cc21 nan
CHEMBL3692900 131681 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1CNCc2c1oc1c(Cl)cc(S(=O)(=O)c3ccccc3)cc21 nan
66801673 112074 0 None -32 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289969 112074 0 None -32 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
66801333 112088 0 None -6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 7 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289982 112088 0 None -6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 7 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
156020306 178129 0 None -26 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 602 11 0 6 6.9 O=S(=O)(c1ccccc1)N(CCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2020.115459
CHEMBL4648390 178129 0 None -26 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 602 11 0 6 6.9 O=S(=O)(c1ccccc1)N(CCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2020.115459
2389 3331 118 None -2570 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
5073 3331 118 None -2570 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
96 3331 118 None -2570 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
CHEMBL85 3331 118 None -2570 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
DB00734 3331 118 None -2570 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
122442272 138348 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138348 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138348 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
155529153 171401 0 None 3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 378 4 1 6 0.3 CC([Se]c1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4462404 171401 0 None 3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 378 4 1 6 0.3 CC([Se]c1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
68115782 132261 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 384 3 1 5 2.6 CN(C)C(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696974 132261 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 384 3 1 5 2.6 CN(C)C(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
155561906 175768 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4583613 175768 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
2398 954 62 None -5 29 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm2011657
2801 954 62 None -5 29 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm2011657
701 954 62 None -5 29 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm2011657
CHEMBL415 954 62 None -5 29 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm2011657
DB01242 954 62 None -5 29 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1021/jm2011657
9947817 5047 0 None -204 9 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105261 5047 0 None -204 9 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
2286 3183 51 None -26 30 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3183 51 None -26 30 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3183 51 None -26 30 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3183 51 None -26 30 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3183 51 None -26 30 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
155561915 176470 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4585051 176470 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596544 176470 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
162673753 183056 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 566 11 1 5 6.5 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4794139 183056 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 566 11 1 5 6.5 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
57400391 69751 0 None -6 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935598 69751 0 None -6 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
9979313 5975 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 4 4.9 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079978 5975 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 4 4.9 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
134130475 142323 0 None -562 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cccc(Cl)c1Cl 10.1016/j.ejmech.2016.09.008
CHEMBL3885471 142323 0 None -562 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cccc(Cl)c1Cl 10.1016/j.ejmech.2016.09.008
145971561 164509 0 None -29 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 444 4 1 4 3.7 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)c(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4214709 164509 0 None -29 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 444 4 1 4 3.7 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)c(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
22330705 117942 8 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 438 3 0 3 5.5 Cc1ccc(Cl)cc1N(C)C(=O)c1cn(-c2ccc(F)cc2F)c(=O)c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403345 117942 8 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 438 3 0 3 5.5 Cc1ccc(Cl)cc1N(C)C(=O)c1cn(-c2ccc(F)cc2F)c(=O)c2ccccc12 10.1016/j.bmcl.2015.03.049
168291906 192030 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 452 8 0 5 4.8 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5201984 192030 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 452 8 0 5 4.8 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
2398 954 62 None -5 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
2801 954 62 None -5 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
701 954 62 None -5 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
CHEMBL415 954 62 None -5 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
DB01242 954 62 None -5 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C nan
627240 94182 9 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 7 2 6 2.5 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL249628 94182 9 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 7 2 6 2.5 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccccc1 10.1016/j.bmcl.2007.09.016
122442272 138348 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 138348 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 138348 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
156014041 177208 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4635363 177208 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2020.115459
72198191 89820 0 None -141 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
CHEMBL2377445 89820 0 None -141 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
155538236 172371 0 None -42 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4476164 172371 0 None -42 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
57403056 70748 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 nan
CHEMBL1950749 70748 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 nan
58258849 128981 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(C#N)c31)C1CCC(C2)N1 nan
CHEMBL3669658 128981 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(C#N)c31)C1CCC(C2)N1 nan
11849796 79741 1 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 229 4 1 2 3.3 NCCc1cccc(Sc2ccccc2)c1 10.1021/jm060469q
CHEMBL211688 79741 1 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 229 4 1 2 3.3 NCCc1cccc(Sc2ccccc2)c1 10.1021/jm060469q
162653138 180400 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 314 5 0 4 3.7 CCCCS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4752004 180400 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 314 5 0 4 3.7 CCCCS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
134136134 144437 0 None -120 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 584 15 1 6 5.5 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3906408 144437 0 None -120 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 584 15 1 6 5.5 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
9904281 47749 28 None -26 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1548 47749 28 None -26 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
118626089 165473 3 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239823 165473 3 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44403086 70297 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 327 2 2 5 2.1 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194360 70297 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 327 2 2 5 2.1 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
118626089 165473 3 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239823 165473 3 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
68109154 131657 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692876 131657 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
11177658 60530 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
CHEMBL175794 60530 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
168279625 191007 0 None -21 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4cccc(Cl)c4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5186688 191007 0 None -21 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4cccc(Cl)c4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
118724645 120600 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361003 120600 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545907 120600 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
44387817 60531 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 6 2 5 3.4 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2n1 10.1021/jm049615n
CHEMBL175798 60531 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 6 2 5 3.4 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2n1 10.1021/jm049615n
CHEMBL5080719 214702 0 None -42 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccccc3o2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
2136365 117927 21 None 3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 0 5 4.5 Cc1ccc(S(=O)(=O)c2nc(N3CCc4ccccc4C3)sc2Cl)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403331 117927 21 None 3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 0 5 4.5 Cc1ccc(S(=O)(=O)c2nc(N3CCc4ccccc4C3)sc2Cl)cc1 10.1016/j.bmcl.2015.03.049
118712404 114158 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 335 2 2 3 4.2 O=C(Nc1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL3329428 114158 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 335 2 2 3 4.2 O=C(Nc1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
44388954 122052 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 331 2 1 3 4.4 CN1CC=C(c2cn(C(=O)Nc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359604 122052 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 331 2 1 3 4.4 CN1CC=C(c2cn(C(=O)Nc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
155543653 173195 0 None 4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1cccc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4522568 173195 0 None 4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1cccc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
71163244 173363 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4527388 173363 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
44401549 133559 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.5 Nc1ccc(CC2=CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL371048 133559 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.5 Nc1ccc(CC2=CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
168282819 191210 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 419 10 4 8 3.1 COc1ccccc1OCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5189520 191210 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 419 10 4 8 3.1 COc1ccccc1OCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
137653850 159045 0 None -66 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4096866 159045 0 None -66 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
1222 1664 49 None -138 33 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
3396 1664 49 None -138 33 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
85 1664 49 None -138 33 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
CHEMBL46516 1664 49 None -138 33 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
DB04842 1664 49 None -138 33 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
12005903 51224 13 None 2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2021.128275
CHEMBL1580288 51224 13 None 2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2021.128275
197033 199152 64 None -15 8 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat recombinant 5HT6 receptorBinding affinity to rat recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 199152 64 None -15 8 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat recombinant 5HT6 receptorBinding affinity to rat recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
162665888 182298 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.7 O=S(=O)(c1ccccc1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4784080 182298 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.7 O=S(=O)(c1ccccc1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
137650127 157534 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)c(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4080086 157534 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)c(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
2891368 94041 10 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 6 1 5 3.0 CN1CCN(c2ccc([N+](=O)[O-])c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL248844 94041 10 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 6 1 5 3.0 CN1CCN(c2ccc([N+](=O)[O-])c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12005903 51224 13 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
CHEMBL1580288 51224 13 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
56593643 65680 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834335 65680 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
2389 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
5073 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
96 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
CHEMBL85 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
DB00734 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
13069627 120613 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361001 120613 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546113 120613 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
17374371 117926 9 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 447 5 1 5 4.7 O=S(=O)(Nc1ccn(Cc2cccc3ccccc23)n1)c1ccc(Br)s1 10.1016/j.bmcl.2015.03.049
CHEMBL3403330 117926 9 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 447 5 1 5 4.7 O=S(=O)(Nc1ccn(Cc2cccc3ccccc23)n1)c1ccc(Br)s1 10.1016/j.bmcl.2015.03.049
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
11316536 201779 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm5003952
CHEMBL606765 201779 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm5003952
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44388931 64114 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180826 64114 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
3028955 135177 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 292 6 0 2 4.0 CN(C)CCc1cn(CCc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
CHEMBL371978 135177 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 292 6 0 2 4.0 CN(C)CCc1cn(CCc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
9799635 18021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)c(C)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126374 18021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)c(C)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
53318111 60088 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642862 60088 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739117 60088 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53323436 60132 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642870 60132 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739585 60132 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
44568061 183594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL480123 183594 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
44568139 192585 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 354 3 0 4 3.3 CCN1CCc2c(n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL521419 192585 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 354 3 0 4 3.3 CCN1CCc2c(n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
155551219 173976 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4541828 173976 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
132525570 163645 0 None -7 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
CHEMBL4204059 163645 0 None -7 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
118654355 191261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5190378 191261 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
90469119 185403 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 4.1 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4861001 185403 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 4.1 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164622997 186131 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 491 14 2 6 4.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4871964 186131 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 491 14 2 6 4.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
134130472 142321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 474 8 1 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885452 142321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 474 8 1 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
137633569 156369 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4066125 156369 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
2906325 154874 11 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 5 1 5 3.5 CC(Nc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-])c1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL400704 154874 11 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 5 1 5 3.5 CC(Nc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-])c1ccccc1 10.1016/j.bmcl.2007.09.016
44403104 72479 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198941 72479 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44435637 89364 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236976 89364 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
164614828 185269 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4858771 185269 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
164624322 186136 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 422 8 1 4 3.9 Cc1cccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4872078 186136 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 422 8 1 4 3.9 Cc1cccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164629020 186302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 470 8 1 5 5.5 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.ejmech.2021.113792
CHEMBL4874512 186302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 470 8 1 5 5.5 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.ejmech.2021.113792
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
127045871 140038 0 None 53 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 446 5 0 7 4.0 Cc1cc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)c(C)s1 10.1016/j.bmcl.2016.04.024
CHEMBL3800251 140038 0 None 53 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 446 5 0 7 4.0 Cc1cc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)c(C)s1 10.1016/j.bmcl.2016.04.024
49836619 18644 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276839 18644 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
24783810 176197 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459371 176197 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
155550351 175123 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4569676 175123 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
57396813 71545 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
11316536 201779 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606765 201779 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
88597039 131641 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 4 4.1 [C-]#[N+]c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692861 131641 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 4 4.1 [C-]#[N+]c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
68108726 131665 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccc(CO)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692884 131665 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccc(CO)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68109100 131683 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 315 2 1 3 4.9 Clc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692902 131683 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 315 2 1 3 4.9 Clc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
44435637 89364 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236976 89364 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
16222656 82040 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 456 3 0 4 5.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165543 82040 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 456 3 0 4 5.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
11595209 94841 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253708 94841 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
25024326 62952 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3F)c2)CC1 10.1021/ml100101u
CHEMBL1785057 62952 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3F)c2)CC1 10.1021/ml100101u
16222449 82030 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165534 82030 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2448158 82030 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
10356663 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
CHEMBL328816 111943 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
132495283 149288 0 None 100 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3944687 149288 0 None 100 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
20765678 93466 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 3 1 5 1.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246077 93466 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 3 1 5 1.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44425708 152911 0 None -3 5 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 468 5 1 3 6.0 CC(C)c1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL397476 152911 0 None -3 5 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 468 5 1 3 6.0 CC(C)c1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
275 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
3246 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
5312144 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
CHEMBL46071 3360 9 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
71151889 118255 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 502 9 1 5 5.0 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409253 118255 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 502 9 1 5 5.0 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.12.045
164608896 184420 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 184420 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
15391752 182330 0 None -6 7 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4784373 182330 0 None -6 7 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
1342 35 49 None -45 19 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
3 35 49 None -45 19 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
CHEMBL277120 35 49 None -45 19 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
66803497 158511 0 None -21 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4091193 158511 0 None -21 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
66800823 112066 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 7 1 7 4.4 Cc1c(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289961 112066 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 7 1 7 4.4 Cc1c(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
66801379 112071 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 8 3.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3289966 112071 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 8 3.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
10324985 76781 8 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76781 8 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76781 8 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
44435193 91225 0 None -7 7 Human 5.9 pKi = 5.9 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL240045 91225 0 None -7 7 Human 5.9 pKi = 5.9 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
90656156 110827 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCCNC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260788 110827 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCCNC2 10.1016/j.bmcl.2014.03.049
162648882 179881 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN(CC(F)(F)F)CC3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4745715 179881 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN(CC(F)(F)F)CC3)cc21 10.1016/j.ejmech.2020.112916
132525569 164049 0 None -16 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 272 3 0 5 2.1 CCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
CHEMBL4208934 164049 0 None -16 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 272 3 0 5 2.1 CCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
155568794 176098 0 None -4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 336 7 3 4 3.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cn[nH]c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4591410 176098 0 None -4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 336 7 3 4 3.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cn[nH]c4)o3)c2c1 10.1016/j.ejmech.2019.111857
13069655 120607 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3360992 120607 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546106 120607 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
24966381 84034 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207385 84034 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
10252130 6099 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080741 6099 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164608823 184466 0 None -64 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 480 9 0 6 4.8 CN1CCN(Cc2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
CHEMBL4846866 184466 0 None -64 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 480 9 0 6 4.8 CN1CCN(Cc2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
2848343 94384 16 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 441 4 0 7 3.7 CN1CCN(c2ccc([N+](=O)[O-])c(-n3nc(-c4ccccc4)c4ccccc4c3=O)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250840 94384 16 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 441 4 0 7 3.7 CN1CCN(c2ccc([N+](=O)[O-])c(-n3nc(-c4ccccc4)c4ccccc4c3=O)c2)CC1 10.1016/j.bmcl.2007.09.016
118724643 120602 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361002 120602 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545933 120602 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
168292191 192024 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
CHEMBL5201892 192024 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
54580394 62628 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 385 4 1 5 3.2 COc1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783606 62628 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 385 4 1 5 3.2 COc1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
68115615 131705 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 424 3 0 5 4.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(c1cccnc1)CC3 nan
CHEMBL3692924 131705 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 424 3 0 5 4.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(c1cccnc1)CC3 nan
11463924 60542 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL175836 60542 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2n1CCN(C)C 10.1021/jm049615n
2274 3173 58 None -23 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 58 None -23 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 58 None -23 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 58 None -23 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 58 None -23 31 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44568064 183015 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 5 0 5 3.7 CCCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL479375 183015 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 5 0 5 3.7 CCCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
162652278 180262 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(-c2ccncc2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4750481 180262 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(-c2ccncc2)c2ccccc21 10.1016/j.ejmech.2020.112916
49836720 18691 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
CHEMBL1277287 18691 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
68109552 131668 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2cccn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692887 131668 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2cccn2)c2oc3c(c2c1)CNCC3 nan
11442097 120497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 442 3 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3csc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL354417 120497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 442 3 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3csc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
1016 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3747 78 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
49836505 18740 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277750 18740 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
155568628 176089 0 None -21 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4591250 176089 0 None -21 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
11166261 60523 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 428 3 0 5 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2csc3ccccc23)CC1 10.1021/jm049615n
CHEMBL175732 60523 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 428 3 0 5 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2csc3ccccc23)CC1 10.1021/jm049615n
5 139 72 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
5202 139 72 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
CHEMBL39 139 72 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
DB08839 139 72 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
44364048 39139 0 None -63 6 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
CHEMBL146942 39139 0 None -63 6 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
134153624 152470 0 None 7 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3971039 152470 0 None 7 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
44441242 93752 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 5 3.2 CN(C)CCNc1cccc2c1OC(C)(C)CN2S(=O)(=O)c1cccc(F)c1 10.1016/j.bmcl.2006.12.093
CHEMBL247325 93752 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 5 3.2 CN(C)CCNc1cccc2c1OC(C)(C)CN2S(=O)(=O)c1cccc(F)c1 10.1016/j.bmcl.2006.12.093
145960299 162320 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 4 1 5 2.7 Clc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164639 162320 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 4 1 5 2.7 Clc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
10541285 67630 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2ccc3cc[nH]c3c2)cc1 10.1021/jm050247c
CHEMBL190468 67630 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2ccc3cc[nH]c3c2)cc1 10.1021/jm050247c
145983751 165505 0 None -251 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1ccnc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240642 165505 0 None -251 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1ccnc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
155568224 176121 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 350 4 1 7 2.2 CN1CCN(c2nc(N)nc(CSc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4591878 176121 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 350 4 1 7 2.2 CN1CCN(c2nc(N)nc(CSc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
145951217 162889 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4173628 162889 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
25263310 184107 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 283 4 1 4 2.4 Cc1c(OCc2cccnc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482573 184107 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 283 4 1 4 2.4 Cc1c(OCc2cccnc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
2389 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
5073 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
96 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
CHEMBL85 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
DB00734 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
2389 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
5073 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
96 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
CHEMBL85 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
DB00734 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
CHEMBL5283557 194217 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 484 6 0 5 4.8 O=C1CC2CCc3ccsc3C2=NN1Cc1ccc(CN2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmc.2023.117256
2775690 93011 53 None -47 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 93011 53 None -47 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
118626169 165575 0 None -177 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242268 165575 0 None -177 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
2906372 94444 9 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.4 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3cccnc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL251201 94444 9 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.4 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3cccnc3)c2)CC1 10.1016/j.bmcl.2007.09.016
2284 3182 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3182 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3182 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3182 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3182 33 None -12 29 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
156019279 177973 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 338 3 0 4 3.5 COc1cc2c3c(c1OC)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4645997 177973 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 338 3 0 4 3.5 COc1cc2c3c(c1OC)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
6473679 42687 29 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
CHEMBL1501353 42687 29 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
57391624 71569 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949972 71569 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963102 71569 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
44591029 190991 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 511 7 0 6 5.6 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(CCCc4ccccc4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518639 190991 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 511 7 0 6 5.6 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(CCCc4ccccc4)CC3)nc12 10.1016/j.bmcl.2008.12.107
2843443 117932 18 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 380 2 0 2 5.3 Brc1ccc2c(c1)c1c3n2CCN(Cc2ccccc2)C3CCC1 10.1016/j.bmcl.2015.03.049
CHEMBL3403336 117932 18 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 380 2 0 2 5.3 Brc1ccc2c(c1)c1c3n2CCN(Cc2ccccc2)C3CCC1 10.1016/j.bmcl.2015.03.049
162652495 180462 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCCCC3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4752848 180462 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCCCC3)cccc21 10.1016/j.ejmech.2020.112916
155536152 172139 0 None 9 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 368 4 1 7 2.1 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4473083 172139 0 None 9 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 368 4 1 7 2.1 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
155546194 173517 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4530840 173517 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
11661320 94112 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 8 1 4 4.7 CN1CCN(c2ccc(OCc3ccccc3)c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL249196 94112 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 8 1 4 4.7 CN1CCN(c2ccc(OCc3ccccc3)c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
58258789 128994 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4cccnc4)c31)C1CCC(C2)N1 nan
CHEMBL3669671 128994 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4cccnc4)c31)C1CCC(C2)N1 nan
155554036 174201 0 None 18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4548041 174201 0 None 18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
127045872 140009 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 431 5 0 8 2.9 Cc1noc(C)c1-c1cc(N2CCN(C)CC2)nc2c1ccn2S(=O)(=O)CC(C)C 10.1016/j.bmcl.2016.04.024
CHEMBL3800055 140009 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 431 5 0 8 2.9 Cc1noc(C)c1-c1cc(N2CCN(C)CC2)nc2c1ccn2S(=O)(=O)CC(C)C 10.1016/j.bmcl.2016.04.024
155559811 174838 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4562787 174838 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
1201549 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 597 24 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
145951815 162816 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 4 1 5 2.2 Fc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172521 162816 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 4 1 5 2.2 Fc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
45488151 196910 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm5003952
CHEMBL566213 196910 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm5003952
58258856 127919 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4ccc(N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664743 127919 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4ccc(N)cc4)ccc31)C1CCC(C2)N1 nan
58258805 127941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(F)c31)C1CCC(C2)N1 nan
CHEMBL3664765 127941 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(F)c31)C1CCC(C2)N1 nan
58258874 128970 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccncc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669647 128970 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccncc45)ccc31)C1CCC(C2)N1 nan
10947658 28702 0 None -11 16 Human 7.9 pKi = 7.9 Binding
Binding affinities against 5-hydroxytryptamine 6 receptorBinding affinities against 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28702 0 None -11 16 Human 7.9 pKi = 7.9 Binding
Binding affinities against 5-hydroxytryptamine 6 receptorBinding affinities against 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
24768515 127507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL366151 127507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1016/j.bmcl.2004.09.003
133 2496 52 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 52 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 52 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 52 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 52 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
44438720 93778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247477 93778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
155562620 175202 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4571045 175202 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
118626129 165642 0 None -12 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243848 165642 0 None -12 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
118654344 191200 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5189331 191200 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
118654437 191972 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1cccc(Br)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5201088 191972 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1cccc(Br)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
118654343 192376 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5207494 192376 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
90469047 186004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 3 1 6 3.6 O=S(=O)(c1ccccc1Br)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4870340 186004 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 3 1 6 3.6 O=S(=O)(c1ccccc1Br)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164614987 184727 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 540 10 2 7 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850546 184727 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 540 10 2 7 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
126720403 162610 0 None 37 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162610 0 None 37 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
134130269 142299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 543 9 1 7 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)C4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885238 142299 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 543 9 1 7 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)C4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
44403060 70576 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194904 70576 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403082 71836 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196926 71836 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
164608896 184420 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 184420 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
10042892 5532 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076583 5532 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164611615 184653 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 3.8 COC(=O)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4849680 184653 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 3.8 COC(=O)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
164625863 186611 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4879036 186611 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
145 140 49 None -7 30 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
1832 140 49 None -7 30 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
CHEMBL7257 140 49 None -7 30 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
DB14010 140 49 None -7 30 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
276 3513 50 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
5312149 3513 50 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
CHEMBL431298 3513 50 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
45488151 196910 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
CHEMBL566213 196910 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
155560922 174989 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 444 4 2 5 4.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4566557 174989 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 444 4 2 5 4.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
24783808 176198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 4 0 6 4.3 CC(C)N1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459372 176198 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 4 0 6 4.3 CC(C)N1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
24783550 176732 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460194 176732 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
155545832 173476 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2c(C3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4530023 173476 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2c(C3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
71502591 118239 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 508 9 1 5 5.6 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409237 118239 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 508 9 1 5 5.6 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
56933434 112097 0 None -21 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289991 112097 0 None -21 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
66801139 112116 0 None -14 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
CHEMBL3290009 112116 0 None -14 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
66801225 112117 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
CHEMBL3290010 112117 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
24768515 127507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/acs.jmedchem.5b00179
CHEMBL366151 127507 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/acs.jmedchem.5b00179
68108531 131667 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692886 131667 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CO)c2oc3c(c2c1)CNCC3 nan
57414522 131695 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COCC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692914 131695 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COCC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25123012 201709 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
CHEMBL606401 201709 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
71449798 84421 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165567 84421 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219895 84421 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
24967457 84022 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207373 84022 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
44435649 145825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL391713 145825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5082267 214795 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.1c00497
44435649 145825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL391713 145825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263349 191582 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2ccccc2F)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL519513 191582 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2ccccc2F)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25117680 200635 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 200635 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
16222871 82053 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 5 4.3 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165556 82053 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 5 4.3 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
11003533 116883 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 4 0 5 3.4 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N(C)C 10.1021/jm010943m
CHEMBL338290 116883 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 4 0 5 3.4 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N(C)C 10.1021/jm010943m
10825266 204367 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 5 0 3 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2C(C)C 10.1021/jm990550b
CHEMBL7173 204367 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 5 0 3 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2C(C)C 10.1021/jm990550b
44327453 107911 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 356 3 1 5 2.8 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N 10.1021/jm030030n
CHEMBL319322 107911 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 356 3 1 5 2.8 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N 10.1021/jm030030n
277 1301 62 None -97 50 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 62 None -97 50 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 62 None -97 50 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 62 None -97 50 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 62 None -97 50 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
56944860 159007 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4096479 159007 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
66801429 159727 0 None -5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 6 2 3 4.5 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4104596 159727 0 None -5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 6 2 3 4.5 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
145983059 165645 0 None -18 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243932 165645 0 None -18 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
53327611 69754 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
66800910 112107 0 None -20 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 437 8 1 6 4.0 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3290000 112107 0 None -20 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 437 8 1 6 4.0 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
92042876 151336 0 None -245 10 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151336 0 None -245 10 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
57403056 70748 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950749 70748 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
145963033 161487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4127861 161487 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
11280771 201798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606871 201798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
11464995 60567 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 446 5 0 6 3.3 COc1ccc(OC)c(S(=O)(=O)N2CCC(N3C(=O)OCc4cccc(C)c43)CC2)c1 10.1021/jm049615n
CHEMBL175980 60567 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 446 5 0 6 3.3 COc1ccc(OC)c(S(=O)(=O)N2CCC(N3C(=O)OCc4cccc(C)c43)CC2)c1 10.1021/jm049615n
57400392 69753 0 None -5 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69753 0 None -5 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
127036953 137515 0 None -13 22 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 137515 0 None -13 22 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44438728 93704 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 6 0 3 3.8 COc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247071 93704 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 6 0 3 3.8 COc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
156013326 177494 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4639400 177494 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
155513247 169760 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 364 7 2 3 4.9 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(F)cc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4438777 169760 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 364 7 2 3 4.9 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(F)cc4)o3)c12 10.1016/j.ejmech.2019.111857
10203339 130470 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL368058 130470 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
68108670 131661 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCCNC3 nan
CHEMBL3692880 131661 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCCNC3 nan
155533850 171892 0 None -43 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccc(Cl)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4469633 171892 0 None -43 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccc(Cl)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
88597033 131627 0 None - 1 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 4 3.5 [C-]#[N+]c1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692847 131627 0 None - 1 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 4 3.5 [C-]#[N+]c1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
72550645 114089 0 None -186 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 114089 0 None -186 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
142601343 185603 0 None -45 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185603 0 None -45 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
2389 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
5073 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
96 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
CHEMBL85 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
DB00734 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
2389 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
5073 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
96 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
CHEMBL85 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
DB00734 3331 118 None -2570 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
137644687 158388 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 523 6 0 5 5.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4089941 158388 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 523 6 0 5 5.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
56944763 112111 0 None -331 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290004 112111 0 None -331 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
68109133 131651 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692870 131651 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
71574212 86284 0 None -147 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312935 86284 0 None -147 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
16026344 22250 4 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 373 2 0 3 5.0 O=S1(=O)c2ccccc2N(Cc2ccc(Cl)cc2F)c2ccccc21 10.1016/j.bmcl.2015.03.049
CHEMBL1323386 22250 4 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 373 2 0 3 5.0 O=S1(=O)c2ccccc2N(Cc2ccc(Cl)cc2F)c2ccccc21 10.1016/j.bmcl.2015.03.049
71462178 81426 0 None -54 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 437 7 1 4 4.8 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
CHEMBL2159469 81426 0 None -54 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 437 7 1 4 4.8 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
134157769 154059 0 None -93 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 2 6 4.7 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCO)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3984541 154059 0 None -93 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 2 6 4.7 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCO)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168276579 190368 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 4 1 5 4.2 COc1cccc(Cn2ccc3c(N4CCC(O)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5177167 190368 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 4 1 5 4.2 COc1cccc(Cn2ccc3c(N4CCC(O)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
49836504 18739 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277749 18739 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
49836506 18747 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
CHEMBL1277834 18747 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
2162 41514 100 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41514 100 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
138691316 174688 0 None -67 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 289 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4559312 174688 0 None -67 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 289 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
44438709 152810 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 7 0 4 2.7 CCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL397380 152810 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 7 0 4 2.7 CCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
49781250 17184 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 673 9 1 9 5.1 COc1ccc(N(S(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256256 17184 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 673 9 1 9 5.1 COc1ccc(N(S(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
164625711 186332 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4874914 186332 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
12051078 112168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL329046 112168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
52912977 127901 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127901 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
12051078 112168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
CHEMBL329046 112168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
21514234 168541 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2006.12.089
CHEMBL435534 168541 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2006.12.089
168268997 189971 0 None -19 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 410 7 3 8 2.4 Nc1nc(N)nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5170808 189971 0 None -19 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 410 7 3 8 2.4 Nc1nc(N)nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
57396850 71524 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71524 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71524 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
71727068 91267 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401934 91267 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401938 91267 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
168274079 190289 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 403 3 0 4 5.1 Clc1cccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5175763 190289 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 403 3 0 4 5.1 Clc1cccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
11716331 154913 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 4 1 5 2.5 CN1CCN(c2ccc(C#N)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL400922 154913 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 4 1 5 2.5 CN1CCN(c2ccc(C#N)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
168295839 192245 0 None -165 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 370 9 3 8 1.8 Nc1nc(N)nc(NCCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5205324 192245 0 None -165 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 370 9 3 8 1.8 Nc1nc(N)nc(NCCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
145985050 165690 0 None -1380 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245263 165690 0 None -1380 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
162663591 181982 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 14 0 5 7.2 C#CCN(C)Cc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4780366 181982 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 14 0 5 7.2 C#CCN(C)Cc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
145961507 161471 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4127652 161471 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
11016205 204768 1 None -107 5 Human 6.9 pKi = 6.9 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
CHEMBL74756 204768 1 None -107 5 Human 6.9 pKi = 6.9 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
56595535 65649 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
CHEMBL1834239 65649 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
155569396 176138 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 279 2 1 2 4.1 CCn1cncc1-c1c[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4592256 176138 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 279 2 1 2 4.1 CCn1cncc1-c1c[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
58258830 127924 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664748 127924 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc(F)c4)ccc31)C1CCC(C2)N1 nan
44568101 191438 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 446 5 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL519299 191438 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 446 5 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
145952652 162414 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)c(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166040 162414 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)c(F)c1 10.1016/j.ejmech.2017.12.053
57325520 71538 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949963 71538 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1962945 71538 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
57395190 69749 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 413 2 1 4 4.3 CC1(C(F)(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935596 69749 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 413 2 1 4 4.3 CC1(C(F)(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
44386718 168539 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3ccccc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL435524 168539 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3ccccc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
86294717 114185 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 300 3 2 2 4.2 CC(Nc1ccc2c(c1)CCNCC2)c1ccccc1Cl 10.1021/jm5003952
CHEMBL3329455 114185 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 300 3 2 2 4.2 CC(Nc1ccc2c(c1)CCNCC2)c1ccccc1Cl 10.1021/jm5003952
52913345 127912 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 395 3 1 5 3.4 CN(C)c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664736 127912 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 395 3 1 5 3.4 CN(C)c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258877 127945 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 410 4 1 5 4.1 CC(C)Oc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664769 127945 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 410 4 1 5 4.1 CC(C)Oc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258851 127946 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccc4)c31)C1CCC(C2)N1 nan
CHEMBL3664770 127946 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccc4)c31)C1CCC(C2)N1 nan
58258795 129015 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669692 129015 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
44389075 64113 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 390 3 1 4 4.0 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180823 64113 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 390 3 1 4 4.0 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
53326022 60141 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642863 60141 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739645 60141 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
155560188 174933 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ncccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4565216 174933 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ncccc2c1 10.1021/acsmedchemlett.6b00056
155537074 172270 0 None 9 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4474618 172270 0 None 9 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c12 10.1016/j.ejmech.2019.111857
90469188 184478 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 434 4 1 6 4.0 CC(C)c1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)cc1 10.1021/acs.jmedchem.1c00224
CHEMBL4847012 184478 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 434 4 1 6 4.0 CC(C)c1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)cc1 10.1021/acs.jmedchem.1c00224
90469252 185027 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 442 3 1 6 4.0 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4855043 185027 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 442 3 1 6 4.0 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
44403070 72422 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL198766 72422 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10141477 140258 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380556 140258 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57393468 69752 0 None -6 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69752 0 None -6 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
44420490 141644 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 0 4 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.08.068
CHEMBL385330 141644 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 0 4 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.08.068
155514459 169869 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.9 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4440402 169869 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.9 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155542461 173142 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 442 5 2 6 3.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4521199 173142 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 442 5 2 6 3.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155566855 176242 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4586353 176242 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594758 176242 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
24763430 62619 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783582 62619 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
23655463 88690 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL235987 88690 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1021/jm070521y
68116185 131699 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.7 COCc1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692918 131699 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.7 COCc1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
58158738 138962 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785231 138962 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
137630083 161044 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4101418 161044 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4116501 161044 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
162644013 181839 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4778418 181839 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
58158719 138991 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785431 138991 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595403 65638 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834227 65638 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
25024144 62956 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785060 62956 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
49799667 10913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10913 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
275 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
3246 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
5312144 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
CHEMBL46071 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
25025118 62965 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 1 5 3.4 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCNCC4)ccc32)cc1 10.1021/ml100101u
CHEMBL1785069 62965 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 1 5 3.4 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCNCC4)ccc32)cc1 10.1021/ml100101u
11338378 60797 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3ccc4ccccc4c3)cccc21 10.1021/jm049615n
CHEMBL176117 60797 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3ccc4ccccc4c3)cccc21 10.1021/jm049615n
162675700 183461 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4799043 183461 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
162661064 181858 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 568 13 0 5 6.8 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4778708 181858 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 568 13 0 5 6.8 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
90656157 110828 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 292 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260789 110828 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 292 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
90656172 110843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260805 110843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
118731505 118113 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 557 9 1 6 5.8 O=C1CCc2ccc(OCCCCN3CCC(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3407518 118113 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 557 9 1 6 5.8 O=C1CCc2ccc(OCCCCN3CCC(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
68281136 112055 0 None -15 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 422 7 1 7 2.8 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289950 112055 0 None -15 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 422 7 1 7 2.8 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
66801455 112069 0 None -34 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 8 2.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289964 112069 0 None -34 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 8 2.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
56944667 112098 0 None -93 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289992 112098 0 None -93 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
11270131 60798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL176134 60798 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL5074880 214339 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2337 3256 77 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3256 77 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3256 77 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3256 77 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3256 77 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
2927683 162202 9 None 2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 8 1 2 6.0 CC(NCCC(Cc1ccccc1)c1ccco1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4162688 162202 9 None 2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 8 1 2 6.0 CC(NCCC(Cc1ccccc1)c1ccco1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.010
145986752 167276 0 None -3 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 167276 0 None -3 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
136118729 93062 0 None -12 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 93062 0 None -12 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
136118616 76248 0 None -14 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 76248 0 None -14 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
10088284 66311 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 334 4 1 4 3.1 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL184884 66311 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 334 4 1 4 3.1 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
164622805 185863 0 None -25 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185863 0 None -25 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
155533648 171885 0 None -10 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 486 9 0 6 4.7 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4469539 171885 0 None -10 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 486 9 0 6 4.7 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
126720412 162921 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 4 1 5 3.8 Cc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4174125 162921 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 4 1 5 3.8 Cc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
13069623 120609 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360994 120609 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546108 120609 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
3042 1414 35 None -51 14 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1414 35 None -51 14 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1414 35 None -51 14 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1414 35 None -51 14 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1414 35 None -51 14 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
2303 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3187 68 None -346 26 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
44403101 71997 0 None -223 6 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL197408 71997 0 None -223 6 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
9949258 137599 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1c2n(c3ccccc13)S(=O)(=O)c1ccccc1-2 10.1016/j.bmcl.2006.08.068
CHEMBL375594 137599 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1c2n(c3ccccc13)S(=O)(=O)c1ccccc1-2 10.1016/j.bmcl.2006.08.068
68108522 131686 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 2 3 3.8 OC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692905 131686 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 2 3 3.8 OC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL5285633 194305 0 None -3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 450 7 0 5 4.2 O=C1CC2CCCc3ccsc3C2=NN1CCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
4098 32505 30 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32505 30 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32505 30 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
164611085 184628 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 373 8 2 4 3.5 O=c1[nH]c2c(OCCNCc3ccccc3)cccc2n1Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4849430 184628 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 373 8 2 4 3.5 O=c1[nH]c2c(OCCNCc3ccccc3)cccc2n1Cc1ccccc1 10.1016/j.ejmech.2021.113792
71727064 102408 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
CHEMBL3039719 102408 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
CHEMBL3216145 102408 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
CHEMBL4802046 214060 0 None -2 2 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT6GPCRScan assay: inhibition of 5-HT6
ChEMBL None None None COc1cc(C(=O)O)ncc1C#Cc1ccccc1NS(=O)(=O)c1cccc2c(N(C)C)ccnc12 10.6019/CHEMBL4800726
57400830 68437 0 None -77 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917358 68437 0 None -77 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
155527359 171238 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 5 2 2 5.1 c1ccc(-c2ccc(NCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4459786 171238 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 5 2 2 5.1 c1ccc(-c2ccc(NCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
57396848 71536 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71536 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71536 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
160510 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL1506260 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL295234 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
118736371 118943 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 6 0 9 2.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423335 118943 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 6 0 9 2.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
164613297 184617 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4849230 184617 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
137652310 157250 0 None -50 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076525 157250 0 None -50 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
11110394 179709 18 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1cc(-c2ccccc2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4743932 179709 18 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1cc(-c2ccccc2)c2ccccc21 10.1016/j.ejmech.2020.112916
164618556 185993 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 479 8 1 5 4.4 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4870158 185993 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 479 8 1 5 4.4 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
56593936 65697 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834352 65697 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593936 65697 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834352 65697 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
155515890 170002 0 None -46 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 414 8 0 4 4.6 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4442385 170002 0 None -46 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 414 8 0 4 4.6 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
155553005 174079 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 2 4 4.7 CC(=O)Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4544414 174079 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 2 4 4.7 CC(=O)Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
90654836 112694 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233667 112694 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304308 112694 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
164614127 185137 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 4.7 Cc1cccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4856695 185137 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 4.7 Cc1cccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
71451455 81418 0 None -8 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 9 1 5 4.1 CSc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159461 81418 0 None -8 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 9 1 5 4.1 CSc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
162668604 182586 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
CHEMBL4788022 182586 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
57394663 71555 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949973 71555 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963031 71555 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
11674694 94813 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL253502 94813 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
58258784 127963 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ncccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664788 127963 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ncccc45)ccc31)C1CCC(C2)N1 nan
90178632 145428 0 None -9 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 468 10 1 5 4.1 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3914155 145428 0 None -9 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 468 10 1 5 4.1 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155538814 173263 0 None 4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4524981 173263 0 None 4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2019.06.022
5280953 97362 109 None -1 8 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
CHEMBL269538 97362 109 None -1 8 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
118626120 165789 0 None -245 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4247770 165789 0 None -245 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
3158 56267 27 None -851 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 56267 27 None -851 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
164615296 185420 0 None -19 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 465 9 0 5 5.6 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCCCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4861311 185420 0 None -19 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 465 9 0 5 5.6 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCCCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
2866185 94341 9 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 286 7 3 5 2.6 NCCNc1ccc([N+](=O)[O-])c(NCc2ccccc2)c1 10.1016/j.bmcl.2007.09.016
CHEMBL250663 94341 9 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 286 7 3 5 2.6 NCCNc1ccc([N+](=O)[O-])c(NCc2ccccc2)c1 10.1016/j.bmcl.2007.09.016
74763017 113719 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
CHEMBL3323289 113719 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
52913098 127906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc(CN)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664730 127906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc(CN)cc4)ccc31)C1CCC(C2)N1 nan
58258820 127961 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccncc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664786 127961 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccncc54)ccc31)C1CCC(C2)N1 nan
58258833 127968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127968 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
10472143 119277 0 None -33 16 Human 7.8 pKi = 7.8 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 119277 0 None -33 16 Human 7.8 pKi = 7.8 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
11849787 139239 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378892 139239 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
1613 2348 53 None -5 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
205 2348 53 None -5 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
3964 2348 53 None -5 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
CHEMBL831 2348 53 None -5 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
DB00408 2348 53 None -5 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
118654431 191618 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5195558 191618 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
164609469 184394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 550 13 2 8 4.1 CCN(C)C(=O)Oc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
CHEMBL4845823 184394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 550 13 2 8 4.1 CCN(C)C(=O)Oc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
134130529 142135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 8 0 6 4.1 CN(CCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3883443 142135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 8 0 6 4.1 CN(CCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
10140915 140355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380772 140355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
46880705 5555 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(Cl)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076687 5555 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(Cl)cc12 10.1016/j.bmcl.2010.01.073
52912973 70749 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70749 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164612119 184632 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 1 5 4.4 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4849477 184632 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 1 5 4.4 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
44420569 84896 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(CCN(C)C)cn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
CHEMBL223637 84896 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(CCN(C)C)cn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
11849787 139239 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
CHEMBL378892 139239 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
155533573 171867 0 None 346 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4469147 171867 0 None 346 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
155537227 172286 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 458 5 2 5 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4474829 172286 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 458 5 2 5 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
127047536 139884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 506 4 0 6 5.0 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCCCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3799330 139884 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 506 4 0 6 5.0 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCCCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
45484307 196829 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565753 196829 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
24771124 184334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484333 184334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
90656167 110838 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 3 3.2 O=C1OC(c2ccccc2F)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260800 110838 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 3 3.2 O=C1OC(c2ccccc2F)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
57396850 71524 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71524 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71524 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
66801613 112050 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289945 112050 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
16222868 82029 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Br)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165533 82029 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Br)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
25263351 184372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1cccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484534 184372 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1cccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
10228179 63357 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 489 6 2 5 5.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCOCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL179492 63357 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 489 6 2 5 5.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCOCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
162650168 180106 0 None -25 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4748379 180106 0 None -25 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
23653133 56684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 3 0 5 3.4 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642415 56684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 3 0 5 3.4 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
25263306 184237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 307 4 1 4 2.9 Cc1c(OCc2cccc(C#N)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483558 184237 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 307 4 1 4 2.9 Cc1c(OCc2cccc(C#N)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL5089348 215203 0 None -7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.1c00497
44395500 122576 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.7 CNCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL360181 122576 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.7 CNCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
10024749 158566 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 5 0 6 2.9 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4091721 158566 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 5 0 6 2.9 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/acs.jmedchem.6b01662
16222447 82026 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165530 82026 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
16222763 82056 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 4 4.6 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165559 82056 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 4 4.6 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
16222761 82022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165526 82022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
275 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
3246 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
5312144 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
CHEMBL46071 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
275 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
3246 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
5312144 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
CHEMBL46071 3360 9 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
164610188 185055 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 185055 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
75306277 109254 0 None -7 23 Human 7.8 pKi = 7.8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109254 0 None -7 23 Human 7.8 pKi = 7.8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
46890294 7161 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 413 5 2 4 3.2 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ncc[nH]1 10.1016/j.bmcl.2010.03.110
CHEMBL1085409 7161 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 413 5 2 4 3.2 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ncc[nH]1 10.1016/j.bmcl.2010.03.110
44425706 150608 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL395525 150608 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
16019553 10706 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10706 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322547 56685 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642416 56685 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL4115766 212927 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL None None None None nan
56944862 156768 0 None -33 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4070715 156768 0 None -33 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
137633644 156554 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 453 5 0 6 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068315 156554 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 453 5 0 6 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
54586997 62538 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782363 62538 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
12005903 51224 13 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
CHEMBL1580288 51224 13 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
90656174 110845 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260807 110845 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
118731504 118236 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 1 4 6.6 O=C1CCc2ccc(OCCCCN3CCC(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409234 118236 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 1 4 6.6 O=C1CCc2ccc(OCCCCN3CCC(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118731506 118237 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 11 2 4 5.6 O=C1CCc2ccc(OCCCCNCCc3cn(Cc4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409235 118237 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 11 2 4 5.6 O=C1CCc2ccc(OCCCCNCCc3cn(Cc4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
160510 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL1506260 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL295234 101127 40 None -5 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
3564 118148 86 None 3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 214 1 1 2 2.5 COc1ccc2c3c([nH]c2c1)C(C)=NCC3 10.1021/acs.jmedchem.0c01887
CHEMBL1494278 118148 86 None 3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 214 1 1 2 2.5 COc1ccc2c3c([nH]c2c1)C(C)=NCC3 10.1021/acs.jmedchem.0c01887
CHEMBL340807 118148 86 None 3 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 214 1 1 2 2.5 COc1ccc2c3c([nH]c2c1)C(C)=NCC3 10.1021/acs.jmedchem.0c01887
156010396 177127 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 392 5 1 4 4.2 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4633765 177127 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 392 5 1 4 4.2 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
90644074 112072 0 None -151 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289967 112072 0 None -151 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
134151118 152201 0 None -72 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 498 12 1 4 5.4 CN(C)Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3968569 152201 0 None -72 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 498 12 1 4 5.4 CN(C)Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
162643605 181701 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccncc3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4776760 181701 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccncc3)cccc21 10.1016/j.ejmech.2020.112916
52912977 127901 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127901 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL5083505 214866 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00497
11384694 128059 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 3 0 5 3.5 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3cccnc23)CC1 10.1021/jm049615n
CHEMBL366515 128059 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 3 0 5 3.5 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3cccnc23)CC1 10.1021/jm049615n
2771422 94079 15 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 5 2 6 2.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1cccnc1 10.1016/j.bmcl.2007.09.016
CHEMBL249032 94079 15 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 5 2 6 2.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1cccnc1 10.1016/j.bmcl.2007.09.016
2247 505 81 None -53 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 81 None -53 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 81 None -53 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 81 None -53 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 81 None -53 42 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
72550642 114078 0 None -173 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 114078 0 None -173 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
57402588 68426 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917347 68426 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
155528725 171390 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 2 2 5.2 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)s2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4462131 171390 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 2 2 5.2 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)s2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4802046 214060 0 None -2 2 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT6GPCRScan assay: inhibition of 5-HT6
ChEMBL None None None COc1cc(C(=O)O)ncc1C#Cc1ccccc1NS(=O)(=O)c1cccc2c(N(C)C)ccnc12 10.6019/CHEMBL4800726
168277941 190683 0 None -72 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 374 9 2 4 1.8 NS(=O)(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5181868 190683 0 None -72 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 374 9 2 4 1.8 NS(=O)(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
57403841 71554 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949968 71554 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963030 71554 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
12017578 108571 21 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2[nH]cc(CCN(C)C)c12 10.1021/jm030030n
CHEMBL32029 108571 21 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2[nH]cc(CCN(C)C)c12 10.1021/jm030030n
68108408 131658 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692877 131658 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
50878551 90745 61 None -2 18 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90745 61 None -2 18 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL5085390 214964 0 None -12 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc3cc(Cl)ccc3c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
21509921 104458 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
145946714 167558 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4213352 167558 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300399 167558 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
57395084 71551 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949964 71551 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963027 71551 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
21509921 104458 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
164610373 185229 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 480 8 2 6 4.0 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4858014 185229 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 480 8 2 6 4.0 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
57396088 70767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950768 70767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 nan
71449644 81441 0 None -15 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 436 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159484 81441 0 None -15 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 436 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
57400477 69741 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935588 69741 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
57396088 70767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950768 70767 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11573559 94842 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 1 2 3 3.7 CC1(c2ccc(N)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253709 94842 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 1 2 3 3.7 CC1(c2ccc(N)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
57398615 71549 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71549 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71549 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
1296368 50821 16 None 1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 458 5 2 5 6.0 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccccc1 10.1016/j.bmcl.2015.03.049
CHEMBL1576791 50821 16 None 1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 458 5 2 5 6.0 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccccc1 10.1016/j.bmcl.2015.03.049
155530285 171491 0 None 20 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 6 1 7 3.9 COc1ccc2c(c1)c(-c1c(C)nc(N)n1CC(F)F)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4463737 171491 0 None 20 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 6 1 7 3.9 COc1ccc2c(c1)c(-c1c(C)nc(N)n1CC(F)F)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
25107716 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
8436 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL522691 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
25107716 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 2351 43 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
7125890 117938 12 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 408 4 1 4 5.8 Cc1ccc(Nc2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403341 117938 12 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 408 4 1 4 5.8 Cc1ccc(Nc2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)cc1 10.1016/j.bmcl.2015.03.049
162670887 182969 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
CHEMBL4793078 182969 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
137632931 156576 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
CHEMBL4068577 156576 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
156016142 177748 0 None -8 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4642594 177748 0 None -8 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
162671683 182890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 559 12 2 6 4.9 C[C@H](NCc1ccc(OCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4792096 182890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 559 12 2 6 4.9 C[C@H](NCc1ccc(OCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
44369599 119698 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 461 5 2 5 2.9 COc1ccc(S(=O)(=O)Nc2c(F)cc(Br)cc2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL347335 119698 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 461 5 2 5 2.9 COc1ccc(S(=O)(=O)Nc2c(F)cc(Br)cc2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
134148634 148523 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
CHEMBL3938498 148523 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
134150535 151623 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3963688 151623 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
134151926 153436 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3979230 153436 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
46889915 7417 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)Cc3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086546 7417 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)Cc3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
24865727 193113 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT6 receptorDisplacement of radioligand from human cloned 5HT6 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 193113 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT6 receptorDisplacement of radioligand from human cloned 5HT6 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
156013801 177282 0 None -93 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 278 1 0 2 3.5 CN(C)c1ccc2c(c1)-c1cccc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4636329 177282 0 None -93 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 278 1 0 2 3.5 CN(C)c1ccc2c(c1)-c1cccc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
72198011 89845 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL2377591 89845 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
315017 205685 109 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 257 2 0 3 2.9 O=S(=O)(c1ccccc1)n1ccc2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL82224 205685 109 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 257 2 0 3 2.9 O=S(=O)(c1ccccc1)n1ccc2ccccc21 10.1016/j.ejmech.2020.112916
72198011 89845 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
CHEMBL2377591 89845 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
118736370 118942 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 7 0 9 2.3 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423334 118942 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 7 0 9 2.3 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
2470 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
2470 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3653 50 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
45488143 197766 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm5003952
CHEMBL571762 197766 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm5003952
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
145 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
1832 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
CHEMBL7257 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
DB14010 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
12147017 166058 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL425714 166058 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
145 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
1832 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
CHEMBL7257 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
DB14010 140 49 None -7 30 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
134131115 142207 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 9 1 6 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884154 142207 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 9 1 6 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130035 154593 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884254 154593 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3991406 154593 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
44403076 71803 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL196792 71803 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
57402187 69750 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69750 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
164610188 185055 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 185055 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
46880531 6299 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081793 6299 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
52942395 17921 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL1259203 17921 0 None -30 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
164619953 185479 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4862131 185479 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113792
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
45488143 197766 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
CHEMBL571762 197766 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
155531455 171653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 452 7 2 6 4.2 CCC(=O)Nc1nc(CC)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4466071 171653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 452 7 2 6 4.2 CCC(=O)Nc1nc(CC)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
23655288 147236 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccccc2I)c2ccccc12 10.1021/jm070521y
CHEMBL392844 147236 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccccc2I)c2ccccc12 10.1021/jm070521y
127047776 139935 0 None 34 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 412 5 0 6 3.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799638 139935 0 None 34 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 412 5 0 6 3.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
90656166 110837 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 308 2 1 3 3.1 O=C1OC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260799 110837 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 308 2 1 3 3.1 O=C1OC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
71151925 118263 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 489 9 0 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409261 118263 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 489 9 0 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
12 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
6918513 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
11372111 201764 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
CHEMBL606706 201764 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
57414392 131622 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692842 131622 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
68108812 131652 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 392 2 1 5 4.3 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)C2CCC(C4)N2)c2ccccc12 nan
CHEMBL3692871 131652 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 392 2 1 5 4.3 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)C2CCC(C4)N2)c2ccccc12 nan
68108636 131674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115683 131730 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692949 131730 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
16222655 82021 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165525 82021 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL5090557 215270 0 None -23 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccccc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
137656063 158691 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4093110 158691 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
56595402 65637 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL5082182 214793 1 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(Cl)c1 10.1021/acs.jmedchem.1c00497
44544596 177425 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 354 3 2 5 2.9 O=S(=O)(Nc1ccc2[nH]ccc2c1)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
CHEMBL4638578 177425 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 354 3 2 5 2.9 O=S(=O)(Nc1ccc2[nH]ccc2c1)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
53327611 69754 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
164619216 185664 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185664 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
44286416 141418 0 None -15 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL38409 141418 0 None -15 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
54582159 62539 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782364 62539 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
58158717 139046 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 415 3 2 3 3.2 CCN/C(=N\S(=O)(=O)c1ccc2[nH]c(C(F)(F)F)cc2c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786071 139046 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 415 3 2 3 3.2 CCN/C(=N\S(=O)(=O)c1ccc2[nH]c(C(F)(F)F)cc2c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
66801354 112083 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289977 112083 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
117209857 185138 1 None -3 8 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 185138 1 None -3 8 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
58622472 181193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccccc3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4761081 181193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccccc3)cccc21 10.1016/j.ejmech.2020.112916
162644220 181773 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 573 13 2 6 5.3 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4777701 181773 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 573 13 2 6 5.3 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
126720427 162544 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 405 4 1 5 3.8 Fc1ccc(-c2nc3c(N4CCNCC4)ccnc3n2Cc2cccc(F)c2)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4168070 162544 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 405 4 1 5 3.8 Fc1ccc(-c2nc3c(N4CCNCC4)ccnc3n2Cc2cccc(F)c2)cc1 10.1016/j.ejmech.2017.12.053
134139826 146532 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3922670 146532 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155538367 172381 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 263 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4476372 172381 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 263 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
134133483 143209 0 None -87 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 614 16 1 7 5.5 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3896355 143209 0 None -87 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 614 16 1 7 5.5 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
3142696 153922 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 2 6 2.8 Cc1ccccc1OCCNc1cc(N2CCNCC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL398336 153922 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 2 6 2.8 Cc1ccccc1OCCNc1cc(N2CCNCC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
10296699 62397 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 9 2 3 5.4 CCN(CC)CCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL177970 62397 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 9 2 3 5.4 CCN(CC)CCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
10113852 63173 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL178985 63173 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
134135516 144173 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3904094 144173 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11559141 154867 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 338 4 1 4 2.6 CC(=O)N(Cc1ccccc1)c1ccc(N2CCN(C)CC2)cc1N 10.1016/j.bmcl.2007.09.016
CHEMBL400660 154867 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 338 4 1 4 2.6 CC(=O)N(Cc1ccccc1)c1ccc(N2CCN(C)CC2)cc1N 10.1016/j.bmcl.2007.09.016
156018383 177923 0 None -134 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2020.115459
CHEMBL4645308 177923 0 None -134 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2020.115459
44413644 80241 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1cccc2c1c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2006.04.094
CHEMBL213800 80241 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1cccc2c1c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2006.04.094
24967097 84028 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 453 4 0 5 4.4 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207379 84028 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 453 4 0 5 4.4 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
126720406 162426 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 393 5 1 6 3.5 COc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166211 162426 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 393 5 1 6 3.5 COc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
126720370 163034 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 409 4 1 6 4.3 Clc1cccc(Cn2c(-c3cccs3)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175926 163034 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 409 4 1 6 4.3 Clc1cccc(Cn2c(-c3cccs3)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
49782361 17177 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 8 6.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(S(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256249 17177 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 8 6.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(S(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
11270546 130890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 3 0 5 3.9 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4cccnc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL368557 130890 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 3 0 5 3.9 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4cccnc34)CC1)C(=O)OC2 10.1021/jm049615n
155533534 171884 0 None -128 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4469537 171884 0 None -128 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
22549784 117937 6 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 418 4 0 4 4.9 COc1cccc(-n2cc(C(=O)N(C)c3cccc(Cl)c3)c3ccccc3c2=O)c1 10.1016/j.bmcl.2015.03.049
CHEMBL3403340 117937 6 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 418 4 0 4 4.9 COc1cccc(-n2cc(C(=O)N(C)c3cccc(Cl)c3)c3ccccc3c2=O)c1 10.1016/j.bmcl.2015.03.049
3303 2244 46 None -2454 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 2244 46 None -2454 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 2244 46 None -2454 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
57393365 71550 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
138691314 164636 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4216263 164636 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
162666007 182282 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 341 3 0 4 3.3 O=S(=O)(N1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4783954 182282 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 341 3 0 4 3.3 O=S(=O)(N1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
57325521 71570 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949977 71570 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1963103 71570 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL5283494 194212 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 408 5 0 5 3.1 O=C1CC2CCc3ccsc3C2=NN1CCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
68115818 131744 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 442 2 0 5 4.3 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4cn(C)c5ccccc45)cc3c2C1 nan
CHEMBL3692963 131744 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 442 2 0 5 4.3 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4cn(C)c5ccccc45)cc3c2C1 nan
154956306 179664 0 None -18 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
CHEMBL4743324 179664 0 None -18 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
145980271 166492 0 None -3 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 166492 0 None -3 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
53325242 57070 0 None -8 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 57070 0 None -8 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
138691314 164636 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1039/C8MD00313K
CHEMBL4216263 164636 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1039/C8MD00313K
10658892 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1016/j.bmcl.2004.01.071
CHEMBL7228 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1016/j.bmcl.2004.01.071
10658892 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm990550b
CHEMBL7228 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm990550b
10658892 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm030030n
CHEMBL7228 204458 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm030030n
53328001 111700 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286592 111700 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
145988693 167166 0 None -66 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 167166 0 None -66 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
42 2063 57 None -2951 18 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
56971 2063 57 None -2951 18 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
CHEMBL8412 2063 57 None -2951 18 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
155544811 176551 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4567345 176551 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4597228 176551 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
145985233 165523 0 None -100 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241050 165523 0 None -100 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
5311507 194815 41 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm2011657
CHEMBL53904 194815 41 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm2011657
53328001 111700 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286592 111700 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
145965840 164016 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 425 5 1 4 3.8 O=C1Nc2ccccc2C12CCN(CCN1CCC(Oc3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4208468 164016 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 425 5 1 4 3.8 O=C1Nc2ccccc2C12CCN(CCN1CCC(Oc3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168293886 192180 0 None -24 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 488 8 0 4 4.5 O=S1(=O)N(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2N1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5204088 192180 0 None -24 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 488 8 0 4 4.5 O=S1(=O)N(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2N1CCC3 10.1016/j.ejmech.2022.114319
53324045 57071 0 None -44 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 57071 0 None -44 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
155522233 170660 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 363 7 2 5 4.7 COc1ccc2occ(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4451494 170660 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 363 7 2 5 4.7 COc1ccc2occ(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
155552054 174011 0 None -36 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)c1 10.1016/j.bmcl.2019.06.029
CHEMBL4542754 174011 0 None -36 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)c1 10.1016/j.bmcl.2019.06.029
52913222 127910 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664734 127910 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258796 127940 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 3.9 CCc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664764 127940 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 3.9 CCc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258806 127965 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127965 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
9800707 204503 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm010943m
CHEMBL72574 204503 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm010943m
11849204 139091 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 306 6 2 4 2.0 COc1ccc(NS(=O)(=O)c2ccccc2)cc1CCN 10.1021/jm060469q
CHEMBL378656 139091 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 306 6 2 4 2.0 COc1ccc(NS(=O)(=O)c2ccccc2)cc1CCN 10.1021/jm060469q
10171 56 18 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
272 56 18 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
CHEMBL274384 56 18 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
16116896 60140 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642861 60140 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739644 60140 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
53320746 60150 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642854 60150 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739685 60150 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
53319443 60154 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642858 60154 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739696 60154 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
118654424 190186 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5174211 190186 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
162676953 183522 0 None 39 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4799851 183522 0 None 39 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
10027518 159663 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103877 159663 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
56595667 65651 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834241 65651 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
135398737 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
38 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
722 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
CHEMBL42 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
DB00363 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
164619216 185664 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185664 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
135398737 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
38 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
722 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
CHEMBL42 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
DB00363 958 93 None -4 89 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
16718822 182658 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL478894 182658 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
155540721 172493 0 None 213 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4483304 172493 0 None 213 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
57398615 71549 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71549 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71549 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
66801018 112092 0 None -6 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 502 8 1 7 4.4 Cc1c(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289986 112092 0 None -6 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 502 8 1 7 4.4 Cc1c(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68108559 131631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692851 131631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
68109199 131653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 2 1 5 4.1 O=S(=O)(c1ccc2oc3c(c2c1)C1CCC(C3)N1)n1ccc2ccc(F)cc21 nan
CHEMBL3692872 131653 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 2 1 5 4.1 O=S(=O)(c1ccc2oc3c(c2c1)C1CCC(C3)N1)n1ccc2ccc(F)cc21 nan
71451605 84420 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165566 84420 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219894 84420 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
56593647 65684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834339 65684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
137636791 155875 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4060415 155875 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/acs.jmedchem.6b01662
57393467 69748 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935595 69748 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
129103313 166753 0 None -1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4283548 166753 0 None -1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
56595404 65639 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
CHEMBL1834228 65639 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
25263327 191686 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.6 Cc1c(C2CCNCC2)ccnc1OCc1cccc(F)c1 10.1016/j.bmcl.2009.03.077
CHEMBL519670 191686 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.6 Cc1c(C2CCNCC2)ccnc1OCc1cccc(F)c1 10.1016/j.bmcl.2009.03.077
56595668 65652 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834242 65652 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
25024146 62957 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCN(C)CC4)ccc32)cc1 10.1021/ml100101u
CHEMBL1785061 62957 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCN(C)CC4)ccc32)cc1 10.1021/ml100101u
25263324 191604 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 343 5 1 2 5.6 CCC(Oc1cccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL519536 191604 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 343 5 1 2 5.6 CCC(Oc1cccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
155567666 176001 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4589391 176001 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
11079889 117468 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 400 6 0 6 2.8 COc1ccc2c(c1)c(CCN1CCOCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL339913 117468 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 400 6 0 6 2.8 COc1ccc2c(c1)c(CCN1CCOCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
134144864 150688 0 None -67 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 600 15 1 7 5.1 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3955917 150688 0 None -67 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 600 15 1 7 5.1 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168284197 190856 0 None -141 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 515 12 4 9 3.6 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5184538 190856 0 None -141 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 515 12 4 9 3.6 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
155534362 171904 0 None -81 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 522 8 1 6 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccccc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
CHEMBL4469813 171904 0 None -81 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 522 8 1 6 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccccc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
168274231 190467 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5178803 190467 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
57396417 71547 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949975 71547 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1963009 71547 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
135449090 189314 4 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL512332 189314 4 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
44393045 161659 0 None -87 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 370 7 3 6 3.6 C[C@H](Nc1nc(N)nc(NCCc2ccc(F)cc2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
CHEMBL413049 161659 0 None -87 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 370 7 3 6 3.6 C[C@H](Nc1nc(N)nc(NCCc2ccc(F)cc2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
11667340 154685 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 344 5 1 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(F)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL399681 154685 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 344 5 1 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(F)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
134151980 153190 0 None -109 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 570 14 1 6 5.1 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3977072 153190 0 None -109 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 570 14 1 6 5.1 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
57396855 71474 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949969 71474 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1962400 71474 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
155551114 176670 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4541606 176670 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598210 176670 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
168279281 191022 0 None -309 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 342 7 3 8 1.1 Nc1nc(N)nc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5186821 191022 0 None -309 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 342 7 3 8 1.1 Nc1nc(N)nc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
24839550 137315 14 None -28 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 137315 14 None -28 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
25263315 173232 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 306 4 1 3 3.9 Cc1c(OCc2cccc(C#N)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL452402 173232 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 306 4 1 3 3.9 Cc1c(OCc2cccc(C#N)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
57393365 71550 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
168287395 191443 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 377 4 1 4 5.1 Clc1cccc(Cn2ccc3c(N[C@H]4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5193046 191443 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 377 4 1 4 5.1 Clc1cccc(Cn2ccc3c(N[C@H]4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
162664825 182089 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CC(F)(F)F)CC3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4781626 182089 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CC(F)(F)F)CC3)cccc21 10.1016/j.ejmech.2020.112916
1355 2011 88 None -125 16 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
142 2011 88 None -125 16 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
CHEMBL478 2011 88 None -125 16 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
DB12110 2011 88 None -125 16 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
49781252 17185 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 744 14 2 9 5.8 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256257 17185 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 744 14 2 9 5.8 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
155546176 173525 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2cc(C3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4531106 173525 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2cc(C3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
145983760 165540 0 None -17 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241497 165540 0 None -17 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44591028 176788 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 5 0 6 4.6 CC(C)CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL460624 176788 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 5 0 6 4.6 CC(C)CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
71460468 81425 0 None -58 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 403 7 1 4 4.2 CC(C)c1ccccc1OCCN1CCC(NC(=O)c2ccc3ccccc3n2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159468 81425 0 None -58 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 403 7 1 4 4.2 CC(C)c1ccccc1OCCN1CCC(NC(=O)c2ccc3ccccc3n2)C1 10.1016/j.ejmech.2012.07.043
90654852 112636 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233675 112636 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302762 112636 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
71454998 81417 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 450 9 1 4 4.5 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159460 81417 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 450 9 1 4 4.5 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
126720448 162537 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4167974 162537 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
44352308 117487 0 None -218 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 117487 0 None -218 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
71458649 81430 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 370 7 1 5 2.3 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159473 81430 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 370 7 1 5 2.3 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
162661003 181398 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccccc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4763575 181398 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccccc3)cc21 10.1016/j.ejmech.2020.112916
168291978 192013 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 482 6 3 7 4.2 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5201719 192013 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 482 6 3 7 4.2 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
71453278 81424 0 None -117 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 7 1 3 4.5 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccc(F)c1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159467 81424 0 None -117 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 7 1 3 4.5 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccc(F)c1F 10.1016/j.ejmech.2012.07.043
69939760 127928 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1ccc2c(ccn2S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664752 127928 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1ccc2c(ccn2S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258791 128991 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128991 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
9905247 107249 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL316881 107249 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
44389091 122020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL359460 122020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
10246789 171008 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1c(S(=O)(=O)c2ccccc2)c2ccccc2n1CCN(C)C 10.1016/j.bmcl.2004.09.003
CHEMBL445652 171008 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1c(S(=O)(=O)c2ccccc2)c2ccccc2n1CCN(C)C 10.1016/j.bmcl.2004.09.003
9905247 107249 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm030030n
CHEMBL316881 107249 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm030030n
2105 3054 37 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3054 37 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3054 37 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3054 37 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3054 37 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
44567984 189220 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL511489 189220 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
155514839 169886 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4440598 169886 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
155519088 170340 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4447200 170340 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
145985527 165709 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245622 165709 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
90469118 184459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1ccc(F)c(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4846691 184459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1ccc(F)c(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469116 184533 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1ccc(F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4847804 184533 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1ccc(F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
155567905 175995 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 566 12 1 5 7.5 Cc1c(OCc2ccccc2)cccc1N1CCN(CCCCCCNc2c3c(nc4c2CCCC4)CCCC3)CC1 10.1016/j.ejmech.2019.07.040
CHEMBL4589118 175995 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 566 12 1 5 7.5 Cc1c(OCc2ccccc2)cccc1N1CCN(CCCCCCNc2c3c(nc4c2CCCC4)CCCC3)CC1 10.1016/j.ejmech.2019.07.040
57400391 69751 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935598 69751 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
46880656 6023 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cccc(F)c12 10.1016/j.bmcl.2010.01.073
CHEMBL1080331 6023 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cccc(F)c12 10.1016/j.bmcl.2010.01.073
46880659 6381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(F)ccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082200 6381 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(F)ccc12 10.1016/j.bmcl.2010.01.073
25024530 62960 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1785064 62960 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
16718919 199781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
CHEMBL593889 199781 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
155569337 176131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 410 5 2 6 3.2 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4592085 176131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 410 5 2 6 3.2 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
24771185 184135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 2 6 3.8 O=S(=O)(c1cccc2ccccc12)n1ncc2ccc(NCC3CCNCC3)cc21 10.1016/j.bmcl.2009.03.071
CHEMBL482756 184135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 2 6 3.8 O=S(=O)(c1cccc2ccccc12)n1ncc2ccc(NCC3CCNCC3)cc21 10.1016/j.bmcl.2009.03.071
56943599 112086 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289980 112086 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
68109169 131654 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3cc(S(=O)(=O)c4ccccc4)ccc3c2C1 nan
CHEMBL3692873 131654 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3cc(S(=O)(=O)c4ccccc4)ccc3c2C1 nan
68115778 132247 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696960 132247 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
16222758 82051 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 3 0 4 4.3 Cc1ccc(S(=O)(=O)n2c3c(c4cc(Cl)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165554 82051 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 3 0 4 4.3 Cc1ccc(S(=O)(=O)n2c3c(c4cc(Cl)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
25123011 201193 0 None 74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 201193 0 None 74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
10094169 156783 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(OC)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4070850 156783 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(OC)ccc32)cc1 10.1021/acs.jmedchem.6b01662
137652249 157112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4074732 157112 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
25263346 184091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482541 184091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
11282389 60822 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 7 2.6 CN(C)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
CHEMBL176218 60822 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 7 2.6 CN(C)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
58158682 138967 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785259 138967 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595666 65650 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834240 65650 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
11362134 63186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL179006 63186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
137643300 158411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 4 1 6 3.1 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090177 158411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 4 1 6 3.1 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
1150 3878 121 None -7 25 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
125 3878 121 None -7 25 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
CHEMBL6640 3878 121 None -7 25 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
DB08653 3878 121 None -7 25 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
44327952 208044 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 208044 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
66801624 156502 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 6 2 3 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4067700 156502 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 6 2 3 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
56944953 159654 0 None -66 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4103725 159654 0 None -66 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
145971527 163117 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 337 7 1 2 5.6 Cc1ccc(C(C)NCCC(c2ccc(F)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4177293 163117 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 337 7 1 2 5.6 Cc1ccc(C(C)NCCC(c2ccc(F)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
24854106 161061 1 None -89 8 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
CHEMBL411663 161061 1 None -89 8 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
53327979 111696 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286589 111696 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
145985958 165610 0 None -151 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4243036 165610 0 None -151 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
155562834 175206 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 450 8 0 5 4.1 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4571077 175206 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 450 8 0 5 4.1 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
137655693 158862 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 285 3 1 7 0.2 CN1CCN(c2nc(N)nc(Cc3ccncc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4094953 158862 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 285 3 1 7 0.2 CN1CCN(c2nc(N)nc(Cc3ccncc3)n2)CC1 10.1016/j.ejmech.2017.04.033
12017576 102978 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL306569 102978 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)c1 10.1016/s0960-894x(00)00453-4
57402187 69750 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69750 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
155519102 170355 0 None 9 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4447416 170355 0 None 9 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164619075 186183 0 None -114 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 413 7 0 5 2.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4872713 186183 0 None -114 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 413 7 0 5 2.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
145961372 161607 0 None -83 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4129589 161607 0 None -83 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
53327979 111696 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286589 111696 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
10563312 204672 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1016/j.bmcl.2004.05.076
CHEMBL7379 204672 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1016/j.bmcl.2004.05.076
10563312 204672 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1021/jm990550b
CHEMBL7379 204672 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1021/jm990550b
59511191 185523 3 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 185523 3 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
71451458 81443 0 None -37 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 5 3.5 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159486 81443 0 None -37 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 5 3.5 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
4725280 173210 3 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 2 2 5.4 Clc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4522860 173210 3 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 2 2 5.4 Clc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155540541 172512 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4483496 172512 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
24829343 159021 0 None -234 9 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 159021 0 None -234 9 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
155569022 176436 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4592962 176436 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596261 176436 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
3561 19077 39 None -3 11 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 19077 39 None -3 11 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
137642134 158341 0 None -131 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4089427 158341 0 None -131 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
73350823 102530 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102530 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102530 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
44443511 154464 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 339 5 1 5 2.8 COC(=O)c1cc(N2CCN(C)CC2)ccc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL399024 154464 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 339 5 1 5 2.8 COC(=O)c1cc(N2CCN(C)CC2)ccc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
156011936 177402 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 8 1 6 4.3 O=c1[nH]c2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4638308 177402 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 8 1 6 4.3 O=c1[nH]c2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
156019026 177796 0 None -38 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 7 4.6 O=c1oc2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4643450 177796 0 None -38 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 7 4.6 O=c1oc2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
44389023 62515 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
CHEMBL178193 62515 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
9841077 9489 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL112024 9489 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
107715 200945 22 None -29 19 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200945 22 None -29 19 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200945 22 None -29 19 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
44567982 179013 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL471099 179013 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
24894055 183168 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL479548 183168 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
44568062 190655 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 370 3 0 5 2.9 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL518153 190655 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 370 3 0 5 2.9 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C)CC3)c1 10.1016/j.bmcl.2008.06.030
44389023 62515 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL178193 62515 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/acsmedchemlett.6b00056
155539600 172859 0 None 21 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 7 2.7 CC(Sc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4515075 172859 0 None 21 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 7 2.7 CC(Sc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
137660291 159408 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4100818 159408 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
11632439 94002 7 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL248658 94002 7 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
53259021 69747 0 None -6 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69747 0 None -6 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
155540796 176356 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4516784 176356 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4595674 176356 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
24763352 62623 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783601 62623 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
57414390 131621 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692841 131621 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCC3 nan
68108422 131673 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 4 2 5 2.8 CC(O)Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692892 131673 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 4 2 5 2.8 CC(O)Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
68108636 131674 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131674 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115647 131704 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 443 4 0 4 5.2 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCC(F)(F)F)CC3 nan
CHEMBL3692923 131704 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 443 4 0 4 5.2 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCC(F)(F)F)CC3 nan
162662399 181929 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4779739 181929 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
25263328 184292 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.5 Cc1c(C2CCNCC2)ccnc1OCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484010 184292 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.5 Cc1c(C2CCNCC2)ccnc1OCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.03.077
44403100 71996 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 384 5 0 5 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL197407 71996 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 384 5 0 5 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL5080305 214677 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1cccc(S(=O)(=O)CC2CCN(CCCc3noc4cc(F)ccc34)C2)c1 10.1021/acs.jmedchem.1c00497
25263344 184151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 3.2 Cc1c(OS(=O)(=O)c2ccccc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482939 184151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 3.2 Cc1c(OS(=O)(=O)c2ccccc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
16222867 81596 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 5 0 6 3.3 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2163369 81596 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 5 0 6 3.3 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
11176859 63305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm049615n
CHEMBL179344 63305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm049615n
17940080 47026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 2 7 2.1 COc1ccc(S(=O)(=O)Nc2cc([N+](=O)[O-])ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154186 47026 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 2 7 2.1 COc1ccc(S(=O)(=O)Nc2cc([N+](=O)[O-])ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9914461 207692 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 514 5 2 6 5.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C(C)C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95504 207692 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 514 5 2 6 5.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C(C)C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
11064294 67953 5 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 2 3 1.8 CCOC(=O)c1[nH]c2ccccc2c1CCN 10.1021/jm050247c
CHEMBL191121 67953 5 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 2 3 1.8 CCOC(=O)c1[nH]c2ccccc2c1CCN 10.1021/jm050247c
44390105 11748 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1181578 11748 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL181877 11748 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
145985289 165707 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cncc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245607 165707 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cncc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44393574 124035 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 189 3 0 1 1.5 CN(C)CC[N+]1=CCc2ccccc21 10.1016/j.bmcl.2004.05.076
CHEMBL363035 124035 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 189 3 0 1 1.5 CN(C)CC[N+]1=CCc2ccccc21 10.1016/j.bmcl.2004.05.076
417052 116855 43 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1021/acs.jmedchem.0c01887
CHEMBL338115 116855 43 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1021/acs.jmedchem.0c01887
2962174 162971 10 None 44 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 410 5 1 4 4.2 O=C1N(Cc2ccccc2)C(c2ccccc2)=NC1(Nc1ccccn1)C(F)(F)F 10.1016/j.ejmech.2018.04.010
CHEMBL4174981 162971 10 None 44 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 410 5 1 4 4.2 O=C1N(Cc2ccccc2)C(c2ccccc2)=NC1(Nc1ccccn1)C(F)(F)F 10.1016/j.ejmech.2018.04.010
90656173 110844 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1ccc(N2CCNCC2)cc1 10.1016/j.bmcl.2014.03.049
CHEMBL3260806 110844 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1ccc(N2CCNCC2)cc1 10.1016/j.bmcl.2014.03.049
13069598 120615 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360998 120615 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546116 120615 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
71727066 91265 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401936 91265 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3215930 91265 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
155567307 175942 0 None -173 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 457 10 0 4 5.6 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4587772 175942 0 None -173 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 457 10 0 4 5.6 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/j.bmcl.2019.06.029
57394332 70766 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950767 70766 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57399092 68434 0 None -75 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 468 9 0 6 3.5 CCN(CCCN1CCN(c2ccccc2OC)CC1)S(=O)(=O)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917355 68434 0 None -75 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 468 9 0 6 3.5 CCN(CCCN1CCN(c2ccccc2OC)CC1)S(=O)(=O)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
57394332 70766 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950767 70766 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 nan
44567932 192070 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL520267 192070 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL5275394 193852 0 None 10 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 601 9 0 8 4.6 O=C1CC2Cc3ccsc3C2=NN1CCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
137657740 159646 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
CHEMBL4103656 159646 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
417052 116855 43 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1016/j.bmcl.2003.09.027
CHEMBL338115 116855 43 None -2 4 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1016/j.bmcl.2003.09.027
137658350 159806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 493 5 0 6 4.1 CSc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4105632 159806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 493 5 0 6 4.1 CSc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
49781469 17187 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 800 18 2 9 7.4 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256259 17187 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 800 18 2 9 7.4 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
11282295 63287 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 8 1 4 4.9 O=S(=O)(CCc1cccc2ccccc12)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm049615n
CHEMBL179264 63287 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 8 1 4 4.9 O=S(=O)(CCc1cccc2ccccc12)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm049615n
168291617 192035 0 None -123 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 413 8 0 6 3.5 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5202054 192035 0 None -123 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 413 8 0 6 3.5 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
90654846 112696 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233672 112696 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304317 112696 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
71726944 102404 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3039669 102404 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3215698 102404 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
162667511 182499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 554 12 0 5 6.4 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4786924 182499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 554 12 0 5 6.4 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
54764323 68438 0 None -151 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
CHEMBL1917359 68438 0 None -151 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
1548955 88581 20 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
2800 88581 20 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
CHEMBL2355051 88581 20 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
24783296 176618 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2nc(N3CCNCC3)oc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
CHEMBL459782 176618 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2nc(N3CCNCC3)oc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
56593644 65681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834336 65681 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
11567716 94678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 1 1 2 4.3 CC1(c2ccccc2)C(=O)Nc2cc(Br)cc(Br)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL252673 94678 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 1 1 2 4.3 CC1(c2ccccc2)C(=O)Nc2cc(Br)cc(Br)c2C1=O 10.1016/j.bmcl.2007.11.045
12017580 207949 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1016/j.bmcl.2004.05.076
CHEMBL97017 207949 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1016/j.bmcl.2004.05.076
12017580 207949 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1021/jm030030n
CHEMBL97017 207949 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1021/jm030030n
21557475 174889 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 442 8 0 5 4.2 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4564093 174889 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 442 8 0 5 4.2 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
164618510 185933 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 4.1 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4869198 185933 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 4.1 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
13069611 120611 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3360995 120611 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546110 120611 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
675366 171788 11 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 1 0 5 2.6 Cc1nc(N2CCCN(C)CC2)c2c3c(sc2n1)CCC3 10.1016/j.ejmech.2019.111857
CHEMBL4467920 171788 11 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 1 0 5 2.6 Cc1nc(N2CCCN(C)CC2)c2c3c(sc2n1)CCC3 10.1016/j.ejmech.2019.111857
156015087 177540 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 406 7 1 4 4.8 C=CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640150 177540 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 406 7 1 4 4.8 C=CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
20923078 117935 6 None 1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 4 2 5 3.2 O=c1ccc(-c2ccc(S(=O)(=O)Nc3cccc4c3CCCC4)s2)n[nH]1 10.1016/j.bmcl.2015.03.049
CHEMBL3403339 117935 6 None 1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 4 2 5 3.2 O=c1ccc(-c2ccc(S(=O)(=O)Nc3cccc4c3CCCC4)s2)n[nH]1 10.1016/j.bmcl.2015.03.049
71455000 81423 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159466 81423 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155527191 171166 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 2 4 4.8 COc1ccc2[nH]cc(CCN(C)Cc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4458840 171166 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 2 4 4.8 COc1ccc2[nH]cc(CCN(C)Cc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
71455000 81423 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1039/C5MD00166H
CHEMBL2159466 81423 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1039/C5MD00166H
134150900 151951 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3966484 151951 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@@H]1CCO 10.1016/j.bmc.2016.10.010
242 470 124 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 470 124 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 470 124 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 470 124 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 470 124 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
22557224 93508 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 452 5 2 7 1.1 CS(=O)(=O)Nc1cccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cccc32)c1 10.1016/j.bmcl.2006.12.093
CHEMBL246289 93508 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 452 5 2 7 1.1 CS(=O)(=O)Nc1cccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cccc32)c1 10.1016/j.bmcl.2006.12.093
164614734 185396 0 None -660 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 443 8 0 6 2.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4860754 185396 0 None -660 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 443 8 0 6 2.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
10257042 204361 0 None -50 7 Human 5.7 pKi = 5.7 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204361 0 None -50 7 Human 5.7 pKi = 5.7 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
44386717 60417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 413 5 1 6 3.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL175068 60417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 413 5 1 6 3.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
67085077 127915 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(NC5CCCC5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664739 127915 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(NC5CCCC5)c4)ccc31)C1CCC(C2)N1 nan
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
44389081 62653 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178385 62653 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44388999 63381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179592 63381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
11739679 169852 0 None 776 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL444015 169852 0 None 776 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
9950402 170454 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL444878 170454 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.05.092
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.05.092
118879893 161203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
CHEMBL4080401 161203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
CHEMBL4117763 161203 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
9902533 133602 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
CHEMBL371292 133602 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.08.006
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.08.006
23844114 207517 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
23844114 207517 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1021/jm030030n
CHEMBL94569 207517 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL94569 207517 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1021/jm030030n
155519559 170381 0 None 15 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4447846 170381 0 None 15 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
155512487 169669 3 None 5 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4437523 169669 3 None 5 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
155565813 175808 0 None 47 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4cc(F)ccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4584504 175808 0 None 47 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4cc(F)ccc34)o2)cc1 10.1016/j.ejmech.2019.111857
90469381 185397 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4860809 185397 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.1c00224
90469319 185688 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 0 6 3.2 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4865309 185688 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 0 6 3.2 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1021/acs.jmedchem.1c00224
90469380 186173 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 440 3 0 6 3.8 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4872586 186173 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 440 3 0 6 3.8 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.1c00224
164617683 184513 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4847532 184513 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
164615023 184792 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 494 12 2 8 3.5 O=[N+]([O-])c1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
CHEMBL4851595 184792 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 494 12 2 8 3.5 O=[N+]([O-])c1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
164620015 185626 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 11 2 6 3.9 Cc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
CHEMBL4864206 185626 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 11 2 6 3.9 Cc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
126720436 180753 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 385 4 1 7 2.2 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL4756098 180753 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 385 4 1 7 2.2 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
162644347 181759 0 None 158 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4777550 181759 0 None 158 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
134130920 142214 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 571 10 1 7 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884195 142214 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 571 10 1 7 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130564 142216 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 12 1 6 5.4 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884227 142216 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 12 1 6 5.4 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134131252 142292 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 621 11 1 7 7.1 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885186 142292 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 621 11 1 7 7.1 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
10073773 161123 16 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4082473 161123 16 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117187 161123 16 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137631027 161145 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4101284 161145 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117309 161145 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44388999 63381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL179592 63381 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
9924959 69464 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193358 69464 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10270799 71772 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 4.0 O=S(=O)(c1cccc(Cl)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196692 71772 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 4.0 O=S(=O)(c1cccc(Cl)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
9902533 133602 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133602 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44433197 88775 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236313 88775 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435603 91750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL240922 91750 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435640 154929 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL401019 154929 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm8009469
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm8009469
155510928 176469 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4435010 176469 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4596543 176469 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
127047901 139633 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 442 6 0 7 3.3 COc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
CHEMBL3797651 139633 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 442 6 0 7 3.3 COc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
10472158 196825 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 196825 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
49836924 18773 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
CHEMBL1278000 18773 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
57400234 71540 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71540 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71540 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
44155874 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668500 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
11463428 201752 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606639 201752 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
11282884 202297 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
CHEMBL610256 202297 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
68108768 131664 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1cccc(C2CCOC2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692883 131664 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1cccc(C2CCOC2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115758 132238 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696951 132238 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
162664339 182128 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4782149 182128 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
44435638 154928 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL401018 154928 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
52913108 70761 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70761 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1007/s00044-004-0121-8
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1007/s00044-004-0121-8
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.05.106
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.05.106
45113400 14231 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099284 14231 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199172 14231 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44435638 154928 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL401018 154928 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57393468 69752 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69752 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.7b00085
6918542 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070910s
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.7b00085
CHEMBL76237 204924 24 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070910s
45484383 196818 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565731 196818 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
45484384 198867 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584049 198867 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263301 184619 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484927 184619 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
44155874 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of 5-HT6 receptor (unknown origin)Inhibition of 5-HT6 receptor (unknown origin)
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00056
CHEMBL1668500 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of 5-HT6 receptor (unknown origin)Inhibition of 5-HT6 receptor (unknown origin)
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00056
68109346 131656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3692875 131656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CCNC3 nan
68115761 132244 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1ccccc1)c1cc(C(F)(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696957 132244 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1ccccc1)c1cc(C(F)(F)F)c2oc3c(c2c1)CNCC3 nan
10026658 156301 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4065437 156301 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44476701 127421 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659968 127421 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
44155874 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57620 22 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44435618 88782 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236334 88782 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
10202564 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
10202564 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
3217 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
3217 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
CHEMBL362628 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
CHEMBL362628 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
44435618 88782 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236334 88782 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
10202564 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
3217 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
CHEMBL362628 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
44554228 18742 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277752 18742 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
45483622 198091 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574403 198091 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
10202564 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
3217 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
CHEMBL362628 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
68115604 131693 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1cccc(-n2cccn2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692912 131693 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1cccc(-n2cccn2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
118010062 131703 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 5 4.2 O=S(=O)(c1ccc(OC(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692922 131703 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 5 4.2 O=S(=O)(c1ccc(OC(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115807 131768 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2ccc(C3CCOC3)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692987 131768 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2ccc(C3CCOC3)cc2)cc2c3c(oc12)CCNC3 nan
11024311 88643 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 341 3 2 5 2.3 CNc1cc(S(=O)(=O)c2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
CHEMBL23575 88643 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 341 3 2 5 2.3 CNc1cc(S(=O)(=O)c2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
9822215 207110 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL92093 207110 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
18180040 68039 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2ccc(I)cc2)cc1N1CCNCC1 10.1021/jm5003952
CHEMBL191429 68039 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2ccc(I)cc2)cc1N1CCNCC1 10.1021/jm5003952
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258779 128985 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 398 3 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(O)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669662 128985 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 398 3 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(O)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
10069592 126353 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 400 8 0 5 3.9 CCCc1c(CCN(C)C)c2cc(OC)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
CHEMBL365040 126353 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 400 8 0 5 3.9 CCCc1c(CCN(C)C)c2cc(OC)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2012.06.002
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2012.06.002
9822215 207110 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2012.06.002
CHEMBL92093 207110 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2012.06.002
16019580 10563 1 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10563 1 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
16117152 60086 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642885 60086 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739101 60086 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2009.04.108
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070521y
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2009.04.108
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070521y
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2007.11.045
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2007.11.045
10067306 198866 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 198866 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
24771120 184100 0 None 56 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 184100 0 None 56 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
155554569 174214 0 None 245 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4548434 174214 0 None 245 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
71151704 118256 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 544 8 1 7 4.4 O=C1CCc2ccc(OCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409254 118256 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 544 8 1 7 4.4 O=C1CCc2ccc(OCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
68115760 131715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.4 O=S(=O)(c1cc(F)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692934 131715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.4 O=S(=O)(c1cc(F)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23625764 147305 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL392899 147305 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44126269 201484 5 None -6 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 201484 5 None -6 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44387089 128807 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 524 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(I)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL366935 128807 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 524 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(I)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44389025 123129 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL361189 123129 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
58258798 129007 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669684 129007 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258802 129014 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669691 129014 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
44389025 123129 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361189 123129 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
9817810 17372 1 None 1 8 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 17372 1 None 1 8 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
23625764 147305 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL392899 147305 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
52913108 70761 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70761 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263339 184169 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 384 4 1 3 5.2 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(Cl)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
CHEMBL482989 184169 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 384 4 1 3 5.2 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(Cl)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
56944666 112113 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290006 112113 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
56943600 112115 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 8 1 5 5.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3290008 112115 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 8 1 5 5.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
68115749 132269 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 132269 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
44438719 93891 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL248071 93891 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
44435614 154450 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL399013 154450 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
137635355 156256 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 300 4 1 4 2.4 NCCc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1021/acs.jmedchem.7b00085
CHEMBL4064950 156256 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 300 4 1 4 2.4 NCCc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1021/acs.jmedchem.7b00085
25263313 172731 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(OCc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL450673 172731 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(OCc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
68115727 131696 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)CCOC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692915 131696 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)CCOC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
17940228 47453 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2ccc(Cl)c(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154525 47453 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2ccc(Cl)c(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354574 47586 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 581 5 2 5 4.2 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154641 47586 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 581 5 2 5 4.2 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369858 47672 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154720 47672 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369855 119812 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL348364 119812 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9805455 208108 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cnc2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc2c1N1CCNCC1 10.1016/s0960-894x(01)00558-3
CHEMBL97899 208108 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cnc2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc2c1N1CCNCC1 10.1016/s0960-894x(01)00558-3
3232 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
3248571 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
CHEMBL60264 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
3232 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
3248571 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
CHEMBL60264 3509 19 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm050247c
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm050247c
6918479 56661 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.12.007
CHEMBL1642114 56661 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.12.007
44435614 154450 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL399013 154450 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
6918542 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.12.007
CHEMBL76237 204924 24 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.12.007
46890158 6459 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 4 1 3 3.4 CN(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082510 6459 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 4 1 3 3.4 CN(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
9822810 69502 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69502 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10293741 71955 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.1 Cn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c21 10.1016/j.bmcl.2005.06.107
CHEMBL197297 71955 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.1 Cn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c21 10.1016/j.bmcl.2005.06.107
22557287 149581 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 3 1 5 2.0 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL394689 149581 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 3 1 5 2.0 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
25024930 62964 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785068 62964 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
24856058 62933 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 461 5 0 5 3.8 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
CHEMBL1784916 62933 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 461 5 0 5 3.8 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
162643812 181663 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4776225 181663 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
25024924 62966 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 5 3.1 O=S(=O)(c1ccc(F)cc1)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785070 62966 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 5 3.1 O=S(=O)(c1ccc(F)cc1)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
3235 3520 15 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
6918553 3520 15 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
CHEMBL329383 3520 15 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
58258867 127922 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 428 3 1 4 5.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664746 127922 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 428 3 1 4 5.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
44389529 131336 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 406 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL368698 131336 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 406 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
49836716 18663 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1277011 18663 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
86302554 110833 0 None 1202 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110833 0 None 1202 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
142592111 175251 0 None 61 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.1 CN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4572260 175251 0 None 61 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.1 CN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
44474631 14082 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197618 14082 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL578631 14082 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
16223065 82037 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 434 4 0 5 4.7 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(Cl)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165540 82037 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 434 4 0 5 4.7 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(Cl)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435604 154861 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL400627 154861 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
52913104 70759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258814 128968 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4cc(F)c5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669645 128968 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4cc(F)c5ccccc54)ccc31)C1CCC(C2)N1 nan
56593645 65682 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834337 65682 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
44435604 154861 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL400627 154861 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57398803 69742 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69742 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69742 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
52913104 70759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70759 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164621197 186249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 5 3.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4873700 186249 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 5 3.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CC3)cccc21 10.1016/j.ejmech.2021.113792
155555402 174375 0 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4551858 174375 0 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
25263355 193665 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2ccc3ccccc3c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL527098 193665 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2ccc3ccccc3c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
68115697 131729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692948 131729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
7184883 10896 3 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10896 3 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
53319441 60099 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642845 60099 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739231 60099 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
56595402 65637 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
46880759 6132 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080899 6132 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
71151757 118259 0 None 27 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 532 10 1 7 4.0 NC(=O)c1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409257 118259 0 None 27 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 532 10 1 7 4.0 NC(=O)c1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
25263322 184308 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484164 184308 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL5077755 214513 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.1c00497
68544798 84523 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL2220317 84523 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL3215892 84523 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
71449795 82042 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165545 82042 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm5003952
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm5003952
58258871 127954 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cnc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664779 127954 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cnc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
58258857 128982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
53320775 60129 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642878 60129 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739546 60129 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53259021 69747 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69747 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
45484399 198964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585098 198964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836824 18711 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277467 18711 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44554227 18750 0 None 33 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18750 0 None 33 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
57398803 69742 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
CHEMBL1935589 69742 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
CHEMBL1949758 69742 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/acs.jmedchem.5b00179
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/acs.jmedchem.5b00179
68115703 131758 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc(C(C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692977 131758 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc(C(C)O)cc2)cc2c3c(oc12)CCNC3 nan
25024727 62970 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/ml100101u
CHEMBL1785074 62970 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/ml100101u
11176859 63305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm5003952
CHEMBL179344 63305 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm5003952
10091667 114161 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 6 1 4 3.6 O=S(=O)(c1cccc(F)c1)c1c[nH]c2c(OCCN3CCCC3)cccc12 10.1021/jm5003952
CHEMBL3329431 114161 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 6 1 4 3.6 O=S(=O)(c1cccc(F)c1)c1c[nH]c2c(OCCN3CCCC3)cccc12 10.1021/jm5003952
58258863 127966 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc5occc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664791 127966 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc5occc5c4)ccc31)C1CCC(C2)N1 nan
6918515 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
71 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
44388955 63086 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178869 63086 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44389086 123749 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362220 123749 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
12147013 65582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL183203 65582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
11747350 107332 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 107332 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
6918515 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
71 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
3950432 169509 8 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 373 5 0 5 4.1 CC(CSc1nc2ccccc2c(=O)n1-c1ccc(Cl)cc1)N(C)C 10.1016/j.ejmech.2019.111857
CHEMBL4434670 169509 8 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 373 5 0 5 4.1 CC(CSc1nc2ccccc2c(=O)n1-c1ccc(Cl)cc1)N(C)C 10.1016/j.ejmech.2019.111857
6918515 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
71 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
11747350 107332 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm030030n
CHEMBL317535 107332 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm030030n
10713238 207826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 355 4 3 4 2.9 CNc1cc(Br)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
CHEMBL96317 207826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 355 4 3 4 2.9 CNc1cc(Br)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
6918515 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
44438732 93892 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 0 2 4.4 CN(C)CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL248085 93892 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 0 2 4.4 CN(C)CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
137644521 158477 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 391 3 1 5 4.1 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1cccc2ccccc12 10.1021/acsmedchemlett.6b00482
CHEMBL4090862 158477 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 391 3 1 5 4.1 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1cccc2ccccc12 10.1021/acsmedchemlett.6b00482
66801537 157932 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4084492 157932 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155515942 170009 0 None 70 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4442456 170009 0 None 70 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
155517413 170176 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
CHEMBL4444655 170176 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
2865 4143 73 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
59 4143 73 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
60854 4143 73 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
CHEMBL708 4143 73 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
DB00246 4143 73 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
121238068 157210 0 None 281 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4076046 157210 0 None 281 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
118654345 190909 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5185190 190909 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
126720425 162114 0 None 34 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161308 162114 0 None 34 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137640158 156774 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 6 0 6 3.2 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4070785 156774 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 6 0 6 3.2 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
44403083 133506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1cccc(Cl)c1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370719 133506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1cccc(Cl)c1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403077 140805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 424 4 1 5 4.0 O=S(=O)(c1ccc(Br)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL381887 140805 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 424 4 1 5 4.0 O=S(=O)(c1ccc(Br)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
16718869 182493 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 486 6 1 4 6.5 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2C1 10.1021/jm8009469
CHEMBL478686 182493 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 486 6 1 4 6.5 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2C1 10.1021/jm8009469
12147013 65582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL183203 65582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
151199471 172839 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2cc(N3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4514440 172839 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2cc(N3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
71151924 118242 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(F)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409240 118242 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(F)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
6918515 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
71 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
68115645 131709 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 2 1 5 3.6 O=S(=O)(c1cncc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692928 131709 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 2 1 5 3.6 O=S(=O)(c1cncc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115677 131725 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692944 131725 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23652993 56694 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 481 4 0 5 4.4 CCN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642425 56694 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 481 4 0 5 4.4 CCN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
16222548 82057 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165560 82057 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
58158668 139028 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785864 139028 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
53327973 111657 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286399 111657 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
44386851 130566 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 6 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL368132 130566 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 6 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
10777767 205071 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 0 3 3.2 CCCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL7732 205071 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 0 3 3.2 CCCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
10757046 107241 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 306 5 4 5 2.2 CNc1cc(NC)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
CHEMBL316855 107241 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 306 5 4 5 2.2 CNc1cc(NC)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
66801561 156077 0 None -660 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4062817 156077 0 None -660 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
66801295 157141 0 None -117 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4075144 157141 0 None -117 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
71451459 81444 0 None -33 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159487 81444 0 None -33 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
10480841 158184 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 492 5 0 7 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc([N+](=O)[O-])cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4087748 158184 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 492 5 0 7 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc([N+](=O)[O-])cc23)CC1 10.1021/acs.jmedchem.6b01662
22028187 197658 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL570971 197658 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
145946527 167570 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4217761 167570 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4300609 167570 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL5071978 214272 0 None -29 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2389 3331 118 None -2570 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 3331 118 None -2570 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 3331 118 None -2570 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 3331 118 None -2570 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 3331 118 None -2570 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
145966418 164241 0 None -36 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3cccc(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4211253 164241 0 None -36 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3cccc(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
13069624 120601 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360991 120601 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545931 120601 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
155539573 172869 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 2 2 5.9 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)o3)cccc2c1 10.1016/j.ejmech.2019.111857
CHEMBL4515249 172869 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 2 2 5.9 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)o3)cccc2c1 10.1016/j.ejmech.2019.111857
144950987 179970 0 None -165 6 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4746800 179970 0 None -165 6 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
71451460 81445 0 None -50 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159488 81445 0 None -50 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
162649787 179976 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1cc(N2CCN(CC(F)(F)F)CC2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4746839 179976 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1cc(N2CCN(CC(F)(F)F)CC2)c2ccccc21 10.1016/j.ejmech.2020.112916
13069603 120608 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360993 120608 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546107 120608 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57402072 71472 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949770 71472 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962398 71472 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
57401516 68399 0 None -63 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 7 1 5 3.0 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL1916746 68399 0 None -63 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 7 1 5 3.0 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
155552799 176305 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4545270 176305 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595236 176305 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
44413645 80154 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1ccc2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
CHEMBL213407 80154 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1ccc2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
59339309 139129 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 351 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1ccc(N(C)C)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786951 139129 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 351 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1ccc(N(C)C)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
118626042 165570 0 None -257 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242170 165570 0 None -257 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
57402070 71563 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71563 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71563 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
155547693 173571 0 None 3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4532712 173571 0 None 3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
164619282 185803 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 387 8 2 4 3.9 Cc1cccc(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4866962 185803 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 387 8 2 4 3.9 Cc1cccc(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
118724648 116465 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361005 116465 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
49836721 18699 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 3 2 5 2.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277375 18699 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 3 2 5 2.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
25263337 184696 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL485016 184696 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
164620748 186245 0 None 5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873623 186245 0 None 5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
58258766 128983 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 417 3 1 6 3.4 COc1cc(S(=O)(=O)c2cncc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669660 128983 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 417 3 1 6 3.4 COc1cc(S(=O)(=O)c2cncc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44390045 12777 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
CHEMBL1187981 12777 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
CHEMBL534698 12777 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
155540673 172533 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 367 2 3 3 2.5 N=C(NC1=NC2CCCCC2C(=O)N1)N1CCC(Cc2ccccc2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4483706 172533 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 367 2 3 3 2.5 N=C(NC1=NC2CCCCC2C(=O)N1)N1CCC(Cc2ccccc2)CC1 10.1016/j.ejmech.2019.111857
11849194 79818 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212063 79818 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
155548677 173728 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.8 COc1ccc2[nH]c(C)c(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4536315 173728 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.8 COc1ccc2[nH]c(C)c(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
126720417 162098 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161125 162098 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
164610456 184500 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4847379 184500 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
53327973 111657 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286399 111657 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
46880533 6172 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 1 4 4.6 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081120 6172 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 1 4 4.6 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
11849194 79818 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL212063 79818 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
44405385 140618 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL381415 140618 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2005.08.059
155523121 170840 0 None 58 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 7 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(NCC(F)F)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4453733 170840 0 None 58 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 7 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(NCC(F)F)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155542237 173090 0 None 56 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 472 7 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4520003 173090 0 None 56 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 472 7 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
23655290 149079 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 318 4 1 4 2.5 NCCc1cn(S(=O)(=O)c2ccc(F)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL394302 149079 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 318 4 1 4 2.5 NCCc1cn(S(=O)(=O)c2ccc(F)cc2)c2ccccc12 10.1021/jm070521y
155551102 173958 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4541473 173958 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
57391618 71469 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71469 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71469 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57391569 71525 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949929 71525 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962864 71525 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
68109184 131633 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2ccccc2c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692853 131633 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2ccccc2c1)c1ccc2oc3c(c2c1)CNCC3 nan
25117679 200604 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 200604 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
10295665 131380 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 4 4.3 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5cccnc45)cc23)CC1 10.1021/jm049615n
CHEMBL368959 131380 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 4 4.3 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5cccnc45)cc23)CC1 10.1021/jm049615n
44403063 71755 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccccc1C(F)(F)F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196661 71755 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccccc1C(F)(F)F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
162665588 182396 0 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
CHEMBL4785434 182396 0 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
56593642 65679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834334 65679 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
44413493 138579 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 386 4 1 6 3.4 COc1cc(OC)c2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
CHEMBL377546 138579 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 386 4 1 6 3.4 COc1cc(OC)c2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
44438718 93853 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 5 0 4 3.3 CN(C)CCc1cn(S(=O)(=O)C2CCCCC2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247872 93853 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 5 0 4 3.3 CN(C)CCc1cn(S(=O)(=O)C2CCCCC2)c2ccccc12 10.1016/j.bmcl.2006.12.089
56944864 157560 0 None -83 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 8 2 3 5.0 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4080369 157560 0 None -83 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 8 2 3 5.0 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
155557143 174550 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 414 7 2 3 6.1 COc1ccc2[nH]cc(CCNCc3ccc(-c4cc(Cl)cc(Cl)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4556193 174550 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 414 7 2 3 6.1 COc1ccc2[nH]cc(CCNCc3ccc(-c4cc(Cl)cc(Cl)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
56944764 112096 0 None -190 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289990 112096 0 None -190 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
127032187 139077 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(OC)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786432 139077 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(OC)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
162647241 179485 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2020.112916
CHEMBL4740955 179485 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2020.112916
127046634 139982 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 449 5 2 4 3.8 COc1cccc(C(C(=O)NC(C)(C)C)N2CCc3c([nH]c4ccccc34)CC2=O)c1OC 10.1016/j.bmcl.2016.03.036
CHEMBL3799903 139982 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 449 5 2 4 3.8 COc1cccc(C(C(=O)NC(C)(C)C)N2CCc3c([nH]c4ccccc34)CC2=O)c1OC 10.1016/j.bmcl.2016.03.036
162675372 183295 0 None -2 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 361 4 0 3 3.5 CN1CCN(CCCN2C(=O)c3ccccc3/C=C\c3ccccc32)CC1 10.1016/j.bmcl.2020.127493
CHEMBL4796968 183295 0 None -2 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 361 4 0 3 3.5 CN1CCN(CCCN2C(=O)c3ccccc3/C=C\c3ccccc32)CC1 10.1016/j.bmcl.2020.127493
71458648 81415 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 4 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159459 81415 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 4 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
90666899 109445 0 None -42 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
CHEMBL3220215 109445 0 None -42 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
1971 2866 38 None -14 30 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm2011657
2404 2866 38 None -14 30 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm2011657
4543 2866 38 None -14 30 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm2011657
CHEMBL445 2866 38 None -14 30 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm2011657
DB00540 2866 38 None -14 30 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1021/jm2011657
45487112 198861 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2nc(Cl)ccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583896 198861 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2nc(Cl)ccc21 10.1016/j.bmcl.2009.10.067
168272182 190406 0 None -4 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5177716 190406 0 None -4 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
49781034 17182 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.0 COc1ccc(N(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256254 17182 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.0 COc1ccc(N(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
145946265 167514 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4203310 167514 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4299892 167514 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
57399091 68423 0 None -57 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2011.09.044
CHEMBL1917344 68423 0 None -57 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2011.09.044
16718826 175407 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 494 7 1 3 6.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2/C1=C\c1ccccc1 10.1021/jm8009469
CHEMBL457569 175407 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 494 7 1 3 6.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2/C1=C\c1ccccc1 10.1021/jm8009469
156009483 177066 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 412 5 1 5 2.8 C#CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4632872 177066 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 412 5 1 5 2.8 C#CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
57393365 71550 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
162676728 183583 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 4.2 O=S(=O)(C1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4800552 183583 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 4.2 O=S(=O)(C1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
155542267 173095 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 475 7 0 6 5.3 CCCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
CHEMBL4520176 173095 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 475 7 0 6 5.3 CCCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
162663493 182002 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4780536 182002 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
162676234 183329 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(N2CCCCC2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4797400 183329 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(N2CCCCC2)c2ccccc21 10.1016/j.ejmech.2020.112916
25263318 191486 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 2 5.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL519359 191486 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 2 5.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
58258847 127942 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(Cl)c31)C1CCC(C2)N1 nan
CHEMBL3664766 127942 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(Cl)c31)C1CCC(C2)N1 nan
58258850 127964 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cnccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664789 127964 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cnccc45)ccc31)C1CCC(C2)N1 nan
155551834 174025 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4543169 174025 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
137642224 158091 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4086515 158091 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
137642224 158091 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2022.114645
CHEMBL4086515 158091 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2022.114645
44403075 71801 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196791 71801 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403053 165964 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1cccc(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL425197 165964 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1cccc(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398717 69744 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935591 69744 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
164612743 184707 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 451 9 1 7 4.0 O=[N+]([O-])c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4850275 184707 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 451 9 1 7 4.0 O=[N+]([O-])c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
137210067 140085 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 428 5 1 7 3.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(O)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800539 140085 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 428 5 1 7 3.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(O)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
22028185 199040 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585931 199040 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836925 18700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277376 18700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
24784325 176187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 385 4 1 6 3.2 CC(C)c1ccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)cc1 10.1016/j.bmcl.2008.12.107
CHEMBL459347 176187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 385 4 1 6 3.2 CC(C)c1ccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)cc1 10.1016/j.bmcl.2008.12.107
24784573 176188 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459348 176188 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
118731502 118234 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 505 9 1 4 6.5 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409232 118234 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 505 9 1 4 6.5 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
66801107 112046 0 None -16 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289709 112046 0 None -16 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
11429601 201777 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606763 201777 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
44155871 60986 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762571 60986 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
57400392 69753 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69753 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
44403090 123981 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL362921 123981 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44438711 93933 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 322 8 0 4 3.1 CCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL248268 93933 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 322 8 0 4 3.1 CCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
66801344 159422 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4100951 159422 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155523771 170909 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 6 2 4 4.5 c1ccc2c(CCNCc3ccc(-c4ccc5c(c4)OCO5)o3)c[nH]c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4454873 170909 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 6 2 4 4.5 c1ccc2c(CCNCc3ccc(-c4ccc5c(c4)OCO5)o3)c[nH]c2c1 10.1016/j.ejmech.2019.111857
71574204 86267 0 None -27 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312640 86267 0 None -27 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
24777063 155578 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@@H]1CCCN1C 10.1021/jm070910s
CHEMBL404421 155578 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@@H]1CCCN1C 10.1021/jm070910s
145963830 164123 0 None -21 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 164123 0 None -21 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
90644075 112079 0 None -34 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 8 1 7 3.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289973 112079 0 None -34 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 8 1 7 3.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
10331436 324 10 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 324 10 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 324 10 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
156012741 177287 0 None -100 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.4 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4636435 177287 0 None -100 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.4 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2020.115459
57396857 71568 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949971 71568 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963101 71568 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
145983794 165654 0 None -18 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cncc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4244280 165654 0 None -18 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cncc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
156019370 177957 0 None -54 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 9 1 5 4.4 O=C(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
CHEMBL4645793 177957 0 None -54 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 9 1 5 4.4 O=C(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
155519599 176313 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4447594 176313 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595274 176313 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
134146185 148837 0 None -50 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2cccnc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3941102 148837 0 None -50 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2cccnc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
24966737 84029 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 4 0 5 3.6 Cc1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207380 84029 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 4 0 5 3.6 Cc1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44155871 60986 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762571 60986 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
162655077 180597 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 580 12 1 5 6.9 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4754407 180597 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 580 12 1 5 6.9 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
2389 3331 118 None -2570 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
5073 3331 118 None -2570 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
96 3331 118 None -2570 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
CHEMBL85 3331 118 None -2570 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
DB00734 3331 118 None -2570 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
11283016 60484 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 7 2 7 3.4 CCN(CC)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
CHEMBL175488 60484 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 7 2 7 3.4 CCN(CC)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
168275185 190656 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 389 3 0 4 4.7 Clc1cccc(Cn2ccc3c(N4CC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5181534 190656 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 389 3 0 4 4.7 Clc1cccc(Cn2ccc3c(N4CC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
71453279 81432 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cc(Cl)ccc2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159475 81432 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cc(Cl)ccc2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
155545088 176657 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4528793 176657 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598089 176657 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
58258760 127969 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 6 3.3 Cn1c2c(c3cc(S(=O)(=O)c4ccc5c(ccn5CCO)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664794 127969 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 6 3.3 Cn1c2c(c3cc(S(=O)(=O)c4ccc5c(ccn5CCO)c4)ccc31)C1CCC(C2)N1 nan
57334553 90475 0 None -758 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1016/j.bmcl.2021.127909
CHEMBL2387229 90475 0 None -758 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1016/j.bmcl.2021.127909
142601337 185970 0 None -72 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 185970 0 None -72 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
58258806 127965 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127965 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
44395570 66259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c2c1 10.1016/j.bmcl.2004.09.003
CHEMBL184640 66259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c2c1 10.1016/j.bmcl.2004.09.003
44341344 9474 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 6 1 5 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL111943 9474 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 6 1 5 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
44567981 189401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1ccc(F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL513051 189401 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1ccc(F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
145984065 165751 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246630 165751 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
155519102 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4447416 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
126720428 182248 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 415 5 1 8 2.2 COc1cccc(S(=O)(=O)n2c(C(C)C)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4783584 182248 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 415 5 1 8 2.2 COc1cccc(S(=O)(=O)n2c(C(C)C)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
46933237 62535 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782360 62535 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
44403073 70324 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 6 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL194465 70324 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 6 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
155519102 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4447416 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164624246 185943 0 None 5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4869411 185943 0 None 5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155522920 170803 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4453250 170803 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
11709684 198617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
CHEMBL578826 198617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
11709684 198617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL578826 198617 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
155552380 174063 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4544099 174063 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
71151591 118252 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2F)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409250 118252 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2F)CC1 10.1016/j.ejmech.2014.12.045
57398615 71549 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71549 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71549 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
56944287 112104 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 9 1 6 4.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289998 112104 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 9 1 6 4.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
66801565 112127 0 None -17 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3290020 112127 0 None -17 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
53325160 56690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 475 4 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642421 56690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 475 4 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2010.11.001
46880756 6027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080380 6027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
24965330 84023 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207374 84023 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2012.10.057
68638941 157742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4082319 157742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
56595529 65645 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
CHEMBL1834234 65645 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
56595529 65645 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
CHEMBL1834234 65645 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
53327974 111689 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286582 111689 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
53328000 111699 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286591 111699 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
11849197 138865 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.4 NCCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378179 138865 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.4 NCCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
23815446 110582 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 443 9 1 6 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL325428 110582 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 443 9 1 6 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
1355 2011 88 None -125 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 2011 88 None -125 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 2011 88 None -125 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 2011 88 None -125 16 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
66801267 112085 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289979 112085 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
136118619 76251 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 76251 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
127045665 140065 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 429 5 1 7 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(=O)[nH]c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800442 140065 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 429 5 1 7 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(=O)[nH]c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
56595408 65644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
CHEMBL1834232 65644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
145982506 165395 0 None -162 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238029 165395 0 None -162 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
162676054 183245 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 587 14 2 6 5.7 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4796358 183245 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 587 14 2 6 5.7 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
164625434 185508 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 8 1 3 4.9 c1ccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4862516 185508 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 8 1 3 4.9 c1ccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
127038033 136606 0 None -33 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 453 8 1 5 4.2 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3ncccc23)CC1 10.1039/C5MD00166H
CHEMBL3739680 136606 0 None -33 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 453 8 1 5 4.2 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3ncccc23)CC1 10.1039/C5MD00166H
162655547 180796 0 None -54 5 Human 4.6 pKi = 4.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4756446 180796 0 None -54 5 Human 4.6 pKi = 4.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
155566439 175798 0 None 12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2019.06.022
CHEMBL4584325 175798 0 None 12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2019.06.022
CHEMBL5284727 194259 0 None 8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 615 9 0 8 5.0 O=C1CC2CCc3ccsc3C2=NN1CCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
57403837 71473 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71473 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71473 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
155520553 176509 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4449590 176509 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596888 176509 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
1472656 34628 25 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1429795 34628 25 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
1472656 34628 25 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1429795 34628 25 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
137633855 156623 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(F)cc3)c2c1 10.1021/acs.jmedchem.6b01662
CHEMBL4069113 156623 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(F)cc3)c2c1 10.1021/acs.jmedchem.6b01662
25263333 179475 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.7 Cc1c(C2CCNCC2)ccnc1OCc1ccc(F)cc1F 10.1016/j.bmcl.2009.03.077
CHEMBL474088 179475 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.7 Cc1c(C2CCNCC2)ccnc1OCc1ccc(F)cc1F 10.1016/j.bmcl.2009.03.077
58258831 128967 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 431 2 1 5 4.2 Cn1c2c(c3cc(S(=O)(=O)n4c5c(c6ccccc64)CCC5)ccc31)C1CCC(C2)N1 nan
CHEMBL3669644 128967 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 431 2 1 5 4.2 Cn1c2c(c3cc(S(=O)(=O)n4c5c(c6ccccc64)CCC5)ccc31)C1CCC(C2)N1 nan
1212 1662 50 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 50 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 50 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 50 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 50 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
53318142 60090 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642867 60090 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739135 60090 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
53322082 60159 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642875 60159 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739701 60159 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44568021 192586 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 410 2 1 4 4.4 O=S(=O)(c1ccc2c(Cl)cccc2c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL521426 192586 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 410 2 1 4 4.4 O=S(=O)(c1ccc2c(Cl)cccc2c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
155518290 170259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4446018 170259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
53327974 111689 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286582 111689 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
53328000 111699 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286591 111699 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
164626757 186294 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 514 9 1 7 5.1 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4874372 186294 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 514 9 1 7 5.1 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.ejmech.2021.113792
127047900 139920 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3C(F)(F)F)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799547 139920 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3C(F)(F)F)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
71151664 118251 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 468 9 1 5 4.4 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409249 118251 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 468 9 1 5 4.4 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
11476019 202299 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 6 2 4 4.3 COc1ccc(Cl)cc1S(=O)(=O)Nc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL610258 202299 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 6 2 4 4.3 COc1ccc(Cl)cc1S(=O)(=O)Nc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm049243i
68115813 132270 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 297 2 1 2 4.3 Clc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696983 132270 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 297 2 1 2 4.3 Clc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
25056080 65690 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834345 65690 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
25056080 65690 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65690 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
56595405 65640 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
70878688 65640 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
CHEMBL1834229 65640 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
16223066 82032 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165536 82032 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
10158456 130092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 409 4 2 4 4.5 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(Cl)s4)cc23)CC1 10.1021/jm049615n
CHEMBL367730 130092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 409 4 2 4 4.5 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(Cl)s4)cc23)CC1 10.1021/jm049615n
25117677 200252 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 200252 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
162650396 180085 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4748107 180085 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
25263348 184370 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccc(Cl)cc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484532 184370 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccc(Cl)cc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
16222962 82033 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.2 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165537 82033 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.2 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
10800458 204355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 0 3 2.8 CCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL7166 204355 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 0 3 2.8 CCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL5094680 215510 0 None -15 8 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
71454999 81422 0 None -794 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159465 81422 0 None -794 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
127040442 136867 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccccc2F)CC1 10.1039/C5MD00166H
CHEMBL3742076 136867 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccccc2F)CC1 10.1039/C5MD00166H
155554556 174397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 452 9 0 4 5.3 CN(CCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2019.07.040
CHEMBL4552323 174397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 452 9 0 4 5.3 CN(CCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2019.07.040
90656171 110842 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 4 1 4 4.2 O=C1OC(c2ccccc2Cl)CN1c1cccc(OC2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260804 110842 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 4 1 4 4.2 O=C1OC(c2ccccc2Cl)CN1c1cccc(OC2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
44396965 12779 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL1187985 12779 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL534703 12779 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
2950739 162963 10 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4174845 162963 10 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
129103161 167070 0 None -51 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4289498 167070 0 None -51 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
10478367 71670 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196370 71670 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL430500 71670 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
137652044 157167 0 None -13 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4075422 157167 0 None -13 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
155561581 175640 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 6 -0.3 CN1CCN(c2nc(N)nc(C[Se]c3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4580959 175640 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 6 -0.3 CN1CCN(c2nc(N)nc(C[Se]c3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
145947937 167723 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4207653 167723 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4302655 167723 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
57403833 71470 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71470 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71470 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
58258825 128964 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 2 5 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5cc[nH]n5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669641 128964 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 2 5 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5cc[nH]n5)c4)ccc31)C1CCC(C2)N1 nan
155543250 173299 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 275 1 1 2 3.3 Cn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4526012 173299 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 275 1 1 2 3.3 Cn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
71453281 81442 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159485 81442 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
90468605 185043 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 266 1 1 3 2.5 CN1CCN(c2nc3ccccc3c3[nH]ccc23)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4855303 185043 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 266 1 1 3 2.5 CN1CCN(c2nc3ccccc3c3[nH]ccc23)CC1 10.1021/acs.jmedchem.1c00224
2855326 94042 13 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccc(OCCNc2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])cc1 10.1016/j.bmcl.2007.09.016
CHEMBL248845 94042 13 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccc(OCCNc2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])cc1 10.1016/j.bmcl.2007.09.016
8447 188949 84 None -33 13 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188949 84 None -33 13 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
138691321 174519 0 None -67 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2c(F)cc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4555349 174519 0 None -67 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2c(F)cc(I)cc12 10.1016/j.ejmech.2019.03.017
44388971 122769 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 428 5 0 4 5.2 O=S(=O)(c1ccccc1)n1cc(C2=CCN(Cc3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL360475 122769 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 428 5 0 4 5.2 O=S(=O)(c1ccccc1)n1cc(C2=CCN(Cc3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
155538451 172387 0 None -9 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 485 10 0 5 5.2 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4476432 172387 0 None -9 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 485 10 0 5 5.2 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
11430512 168279 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 3 0 4 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL433979 168279 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 3 0 4 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
155533990 171875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 461 6 0 6 4.9 CCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
CHEMBL4469325 171875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 461 6 0 6 4.9 CCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
155568249 176109 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4cccc(OC)c34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4591630 176109 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4cccc(OC)c34)o2)c1 10.1016/j.ejmech.2019.111857
71456782 81436 0 None -27 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 364 7 1 4 2.3 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159479 81436 0 None -27 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 364 7 1 4 2.3 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
67268994 163968 2 None -7 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163968 2 None -7 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
57396419 71542 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949976 71542 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1962961 71542 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
44395664 66760 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
CHEMBL185850 66760 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
10017687 67281 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL188182 67281 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
9905247 107249 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm010943m
CHEMBL316881 107249 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm010943m
155516118 170039 3 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 3 4 4.0 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4442855 170039 3 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 3 4 4.0 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
44240802 139181 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787508 139181 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
2771419 154741 24 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 5 2 6 2.2 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccco1 10.1016/j.bmcl.2007.09.016
CHEMBL399962 154741 24 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 5 2 6 2.2 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccco1 10.1016/j.bmcl.2007.09.016
44403074 70288 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 4 1 5 3.9 O=S(=O)(c1ccc(Cl)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194311 70288 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 4 1 5 3.9 O=S(=O)(c1ccc(Cl)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
155518159 170276 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4446215 170276 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
10017687 67281 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL188182 67281 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
24784575 176714 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
CHEMBL459989 176714 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
155565138 175544 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4578632 175544 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
155566852 175882 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4586276 175882 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
56943695 112122 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290015 112122 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68108636 131674 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131674 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115684 131732 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692951 131732 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
10069527 158929 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4095670 158929 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
17940185 119588 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C(F)(F)F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346227 119588 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C(F)(F)F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918576 207715 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 436 4 2 5 3.8 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(01)00558-3
CHEMBL95628 207715 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 436 4 2 5 3.8 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(01)00558-3
9905247 107249 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm050247c
CHEMBL316881 107249 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm050247c
134132432 144740 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3908917 144740 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
46889857 7092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 5 1 5 3.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCCC2CNc1ncccn1 10.1016/j.bmcl.2010.03.110
CHEMBL1085112 7092 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 5 1 5 3.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCCC2CNc1ncccn1 10.1016/j.bmcl.2010.03.110
17978385 71704 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1ccc2ccccc2c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196524 71704 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1ccc2ccccc2c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10149997 127526 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)nccc12 10.1016/j.bmcl.2005.06.107
CHEMBL366248 127526 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)nccc12 10.1016/j.bmcl.2005.06.107
44425703 86667 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 417 4 1 4 4.1 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(C#N)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231640 86667 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 417 4 1 4 4.1 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(C#N)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
11163741 142105 5 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNCC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL388247 142105 5 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNCC3)cc1 10.1016/j.bmcl.2006.10.036
53323873 56699 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 453 4 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642430 56699 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 453 4 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
53327999 111698 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286590 111698 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
66801425 157186 0 None -83 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4075673 157186 0 None -83 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
66801837 157528 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 507 8 2 3 6.1 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4079972 157528 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 507 8 2 3 6.1 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
137654666 158616 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4092243 158616 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
2845118 154083 10 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 3 0 6 2.1 Cc1cc(C)n(-c2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
CHEMBL398482 154083 10 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 3 0 6 2.1 Cc1cc(C)n(-c2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
155515416 176604 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4442148 176604 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4597708 176604 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
56944859 112108 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290001 112108 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
2928642 162289 9 None 3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 7 1 2 6.1 Cc1ccc(C(CCNC(C)c2ccc(Cl)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4164143 162289 9 None 3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 7 1 2 6.1 Cc1ccc(C(CCNC(C)c2ccc(Cl)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
90654844 112624 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233671 112624 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302598 112624 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
44398569 69158 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 458 9 1 5 3.9 CC[N+](C)(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1021/jm050247c
CHEMBL192435 69158 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 458 9 1 5 3.9 CC[N+](C)(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1021/jm050247c
127031619 139032 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 406 4 2 4 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(O)cc1 10.1016/j.bmcl.2016.02.001
CHEMBL3785894 139032 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 406 4 2 4 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(O)cc1 10.1016/j.bmcl.2016.02.001
6623 163321 98 None - 1 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL418971 163321 98 None - 1 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
76284193 146597 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 444 10 1 5 3.6 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1016/j.ejmech.2016.05.005
CHEMBL3923145 146597 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 444 10 1 5 3.6 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1016/j.ejmech.2016.05.005
156021059 178137 0 None -50 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 8 3.5 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)nc2ccccn12 10.1016/j.bmc.2020.115459
CHEMBL4648581 178137 0 None -50 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 8 3.5 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)nc2ccccn12 10.1016/j.bmc.2020.115459
68108826 131680 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 418 3 1 5 3.2 CN(C)C(=O)C1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692899 131680 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 418 3 1 5 3.2 CN(C)C(=O)C1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
44403079 135227 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 312 2 1 4 2.5 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
CHEMBL372373 135227 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 312 2 1 4 2.5 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
44568104 184055 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482260 184055 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
4301799 124805 12 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 222 2 2 1 3.3 Nc1ccc(Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL364248 124805 12 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 222 2 2 1 3.3 Nc1ccc(Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmcl.2005.02.070
118626208 165553 0 None -416 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241830 165553 0 None -416 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
2232766 161371 7 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4126145 161371 7 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
126720445 162215 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4162914 162215 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
155558380 174767 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2ccc(C3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4561144 174767 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2ccc(C3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
163409061 192189 3 None -74 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 456 8 1 6 3.2 O=C(NCCCCCCn1nc2ccccn2c1=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5204274 192189 3 None -74 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 456 8 1 6 3.2 O=C(NCCCCCCn1nc2ccccn2c1=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
86288950 112643 0 None -537 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233666 112643 0 None -537 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302931 112643 0 None -537 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
162650377 180033 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 250 3 0 2 3.8 CN(C)c1cccc2c1ccn2Cc1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4747483 180033 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 250 3 0 2 3.8 CN(C)c1cccc2c1ccn2Cc1ccccc1 10.1016/j.ejmech.2020.112916
1971 2866 38 None -14 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 38 None -14 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 38 None -14 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 38 None -14 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 38 None -14 30 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
71574210 86283 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312934 86283 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
181743 178572 5 None -128 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 178572 5 None -128 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
11681803 155108 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 348 2 2 3 4.1 CNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL401969 155108 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 348 2 2 3 4.1 CNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
71451457 81427 0 None -16 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 394 8 1 5 3.3 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccs2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159470 81427 0 None -16 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 394 8 1 5 3.3 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccs2)C1 10.1016/j.ejmech.2012.07.043
162648387 179877 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 594 13 1 5 7.3 C#CCNC1CCc2c(OCCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4745652 179877 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 594 13 1 5 7.3 C#CCNC1CCc2c(OCCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
74763017 113719 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
CHEMBL3323289 113719 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
197033 199152 64 None -3 8 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1021/jm5003952
CHEMBL589390 199152 64 None -3 8 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1021/jm5003952
9952250 204960 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1021/jm010943m
CHEMBL76466 204960 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1021/jm010943m
197033 199152 64 None -3 8 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptorBinding affinity to human recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 199152 64 None -3 8 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptorBinding affinity to human recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
2726 919 68 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 68 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 68 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 68 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 68 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155554462 174601 0 None 7 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 316 4 1 7 1.5 CN1CCN(c2nc(N)nc(CSc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4557247 174601 0 None 7 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 316 4 1 7 1.5 CN1CCN(c2nc(N)nc(CSc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
145950947 162783 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 3 1 5 2.5 Cc1cccc(Cn2c(C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172073 162783 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 3 1 5 2.5 Cc1cccc(Cn2c(C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
3643745 94043 4 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 370 7 1 6 3.1 Cc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL248846 94043 4 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 370 7 1 6 3.1 Cc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
44403087 133130 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370306 133130 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
164620867 185642 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864448 185642 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
53327999 111698 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286590 111698 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
164616796 184887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4852840 184887 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
44405369 72436 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 4 2 5 3.0 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL198797 72436 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 4 2 5 3.0 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2005.08.059
44474470 14061 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL1197489 14061 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL573981 14061 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
56944190 112100 0 None -5 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 499 8 1 5 5.2 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289994 112100 0 None -5 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 499 8 1 5 5.2 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
66801120 112114 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 7 1 5 5.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3290007 112114 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 7 1 5 5.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
57414520 131694 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1ccc(-n2cccn2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692913 131694 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1ccc(-n2cccn2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414658 131710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 348 2 1 5 3.0 O=S(=O)(c1cccnc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692929 131710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 348 2 1 5 3.0 O=S(=O)(c1cccnc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25263345 173776 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL453732 173776 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
49799685 10951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173209 10951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL5087742 215116 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2csc3ccccc23)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
162652285 180275 0 None -15 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4750664 180275 0 None -15 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
56595670 65677 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834332 65677 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
164611003 185344 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 185344 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
11833220 16765 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 292 5 1 2 3.5 CN(C)CCc1cccc2[nH]c(C(=O)c3ccccc3)cc12 10.1021/jm010943m
CHEMBL124382 16765 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 292 5 1 2 3.5 CN(C)CCc1cccc2[nH]c(C(=O)c3ccccc3)cc12 10.1021/jm010943m
4713248 207907 3 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 207907 3 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
145964159 164329 0 None -56 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 164329 0 None -56 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
71463518 85298 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 237 3 2 2 2.7 NCCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260376 85298 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 237 3 2 2 2.7 NCCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
15256441 181017 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4759121 181017 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
164615095 184947 0 None -204 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 414 7 0 6 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4853700 184947 0 None -204 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 414 7 0 6 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2021.128028
155545526 173399 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4528162 173399 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
134152583 153177 0 None -10 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2cccnc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3976948 153177 0 None -10 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2cccnc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
155554246 174950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 315 6 3 1 4.5 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)[nH]2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4565614 174950 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 315 6 3 1 4.5 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)[nH]2)cc1 10.1016/j.ejmech.2019.111857
72198014 89818 0 None -8 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 484 7 2 4 4.8 COc1ccc2[nH]cc(C3CCN(CCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
CHEMBL2377443 89818 0 None -8 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 484 7 2 4 4.8 COc1ccc2[nH]cc(C3CCN(CCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
57393877 68429 0 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917350 68429 0 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.09.044
137652210 157496 0 None 19 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 375 3 0 5 4.0 O=CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4079631 157496 0 None 19 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 375 3 0 5 4.0 O=CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
4723679 171754 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 384 6 2 2 6.1 Clc1cc(Cl)cc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4467393 171754 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 384 6 2 2 6.1 Clc1cc(Cl)cc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
49782362 17178 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 783 15 2 9 7.6 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256250 17178 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 783 15 2 9 7.6 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
155543223 173298 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2c(N3CCN(C4CCC4)CC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4525992 173298 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2c(N3CCN(C4CCC4)CC3)cccc21 10.1016/j.bmcl.2016.07.055
164618208 185385 0 None -2630 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 467 6 0 5 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4860626 185385 0 None -2630 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 467 6 0 5 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
71456781 81428 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159471 81428 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
164610188 185055 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 185055 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
145974189 164626 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 434 9 1 4 4.2 CC(C)c1ccccc1OCCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
CHEMBL4216126 164626 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 434 9 1 4 4.2 CC(C)c1ccccc1OCCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
117209864 186034 1 None -1 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 186034 1 None -1 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
145962275 161656 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 373 3 1 3 5.3 Clc1cccc(Cn2cc(C3=CCNCC3)c3ccc4cccnc4c32)c1 10.1016/j.bmc.2018.05.033
CHEMBL4130316 161656 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 373 3 1 3 5.3 Clc1cccc(Cn2cc(C3=CCNCC3)c3ccc4cccnc4c32)c1 10.1016/j.bmc.2018.05.033
58258806 127965 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127965 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
44389010 63269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179173 63269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44395499 66926 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 318 4 1 4 2.6 NCCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
CHEMBL186585 66926 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 318 4 1 4 2.6 NCCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
23872163 110479 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 385 6 1 5 2.9 CC(=O)Nc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL324766 110479 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 385 6 1 5 2.9 CC(=O)Nc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/s0960-894x(03)00612-7
53325577 60158 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642874 60158 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739700 60158 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44389010 63269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL179173 63269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
22015412 180528 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4753562 180528 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
11638206 94343 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 4 0 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(Oc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250677 94343 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 4 0 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(Oc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
164611003 185344 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 185344 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164622054 186194 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 0 5 4.4 CN(CCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1)Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4872905 186194 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 0 5 4.4 CN(CCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1)Cc1ccccc1 10.1016/j.ejmech.2021.113792
49780586 17180 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 9 6.1 COc1ccc(N(S(=O)(=O)c2sc3ccc(Cl)cc3c2C)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256252 17180 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 9 6.1 COc1ccc(N(S(=O)(=O)c2sc3ccc(Cl)cc3c2C)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
49836719 18690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
CHEMBL1277286 18690 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
57396813 71545 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
66800909 112070 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 8 3.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3289965 112070 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 8 3.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
56944082 112078 0 None -269 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289972 112078 0 None -269 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68108968 131676 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 2 1 4 4.3 CC1(C)NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692895 131676 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 2 1 4 4.3 CC1(C)NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
24967096 84025 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207376 84025 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
56595669 65653 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834243 65653 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
162666034 182311 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4784228 182311 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
9983033 156126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4063362 156126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1021/acs.jmedchem.6b01662
44397550 71192 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL188285 71192 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL195621 71192 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
24855787 65634 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834221 65634 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
71463519 85299 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 265 4 1 2 3.3 CN(C)CCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260377 85299 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 265 4 1 2 3.3 CN(C)CCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
1984087 162297 10 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 3 5.3 COc1cc(CNCCC2=CCCCC2)ccc1OCc1ccccc1 10.1016/j.ejmech.2018.04.010
CHEMBL4164250 162297 10 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 3 5.3 COc1cc(CNCCC2=CCCCC2)ccc1OCc1ccccc1 10.1016/j.ejmech.2018.04.010
594590 72850 95 None -39 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL200234 72850 95 None -39 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1016/j.bmcl.2005.08.059
90645147 112176 0 None -13 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL3290576 112176 0 None -13 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
71456784 81449 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159492 81449 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
44403085 133550 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.8 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370935 133550 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.8 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
73213195 104459 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
164612518 185394 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4860719 185394 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
73213195 104459 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL508338 188966 0 None -95 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
57398619 71566 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949962 71566 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963099 71566 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
71451454 81412 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 398 8 1 5 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159456 81412 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 398 8 1 5 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
127039755 136653 0 None -45 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 470 8 1 4 4.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1039/C5MD00166H
CHEMBL3740055 136653 0 None -45 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 470 8 1 4 4.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1039/C5MD00166H
16718916 182661 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL478896 182661 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2C1 10.1021/jm8009469
168292411 191890 0 None -34 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 8 2.8 Nc1nc(NCCc2c[nH]c3ccccc23)nc(NCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5199820 191890 0 None -34 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 8 2.8 Nc1nc(NCCc2c[nH]c3ccccc23)nc(NCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
137648205 157877 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 370 4 0 6 2.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ncccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4083953 157877 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 370 4 0 6 2.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ncccc23)CC1 10.1021/acs.jmedchem.6b01662
24968180 84019 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(Br)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207367 84019 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(Br)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
117209971 186485 1 None -5 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 186485 1 None -5 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
168283609 191237 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 418 10 5 8 3.1 COc1ccccc1NCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5190020 191237 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 418 10 5 8 3.1 COc1ccccc1NCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
9841077 9489 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL112024 9489 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1016/s0960-894x(03)00612-7
137635185 155857 0 None 60 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 382 6 0 5 4.0 CCN(CC)CC1=Cc2cn(S(=O)(=O)c3ccccc3)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4060194 155857 0 None 60 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 382 6 0 5 4.0 CCN(CC)CC1=Cc2cn(S(=O)(=O)c3ccccc3)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
16116897 60127 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642876 60127 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739544 60127 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
137658424 159720 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4104479 159720 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
155519102 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4447416 170355 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
2771410 154986 36 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 2 5 2.6 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL401294 154986 36 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 2 5 2.6 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
155550580 174282 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.5 CCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4549734 174282 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.5 CCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
57393365 71550 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71550 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71550 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
68109417 131670 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cn[nH]c2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692889 131670 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cn[nH]c2)c2oc3c(c2c1)CNCC3 nan
137640966 157076 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Cl)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4074234 157076 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Cl)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
25024148 62953 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 5 0 5 3.7 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785058 62953 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 5 0 5 3.7 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
11574113 94742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 3 2 3 4.5 CCNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL253095 94742 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 3 2 3 4.5 CCNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
58158707 139048 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786087 139048 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
16019573 10994 10 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173579 10994 10 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
9921064 127178 25 None 8 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counterDisplacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counter
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 127178 25 None 8 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counterDisplacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counter
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
53327976 111693 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286586 111693 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
25263352 184131 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL482748 184131 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
16222654 82058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165561 82058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
44438708 93407 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 0 4 2.3 CCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL245806 93407 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 0 4 2.3 CCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
56944951 156637 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4069237 156637 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
155538716 173260 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 434 3 0 6 3.8 CC(=O)N1CCCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4524906 173260 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 434 3 0 6 3.8 CC(=O)N1CCCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
1524 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2181 96 None -269 52 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
127026750 137677 0 None -14 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 O=S(=O)(NC1CCN(CCOc2ccccc2C2CCCC2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3758591 137677 0 None -14 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 O=S(=O)(NC1CCN(CCOc2ccccc2C2CCCC2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
134147935 149689 0 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3947670 149689 0 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168290061 191334 0 None -56 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 424 8 3 8 2.7 Nc1nc(N)nc(NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5191557 191334 0 None -56 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 424 8 3 8 2.7 Nc1nc(N)nc(NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
90654672 110093 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 9 1 5 3.5 CSc1ccccc1N1CCN(CCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3235744 110093 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 9 1 5 3.5 CSc1ccccc1N1CCN(CCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
44403078 71412 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 4 1 5 5.3 Cc1c(S(=O)(=O)n2cc(C[C@H]3CCCN3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL195922 71412 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 4 1 5 5.3 Cc1c(S(=O)(=O)n2cc(C[C@H]3CCCN3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
57392612 70754 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70754 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
11849198 139056 33 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 248 3 2 3 2.1 Nc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378618 139056 33 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 248 3 2 3 2.1 Nc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
168279047 191185 0 None -2818 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 437 8 0 8 2.7 O=c1n(CCCCCCN2CCN(c3cccc4c3OCCO4)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5189101 191185 0 None -2818 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 437 8 0 8 2.7 O=c1n(CCCCCCN2CCN(c3cccc4c3OCCO4)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
145965668 164114 0 None -11 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3Cl)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4209807 164114 0 None -11 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3Cl)CC1)C2 10.1016/j.bmcl.2018.06.019
168281784 190947 0 None -47 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 429 8 0 6 4.0 O=c1n(CCCCCCN2CCN(c3cccc4ccccc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5185787 190947 0 None -47 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 429 8 0 6 4.0 O=c1n(CCCCCCN2CCN(c3cccc4ccccc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
44403102 71732 0 None -102 6 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196598 71732 0 None -102 6 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
90654858 112700 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233678 112700 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304355 112700 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
139488606 170757 1 None -724 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(I)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4452569 170757 1 None -724 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(I)c(F)c12 10.1016/j.ejmech.2019.03.017
137630865 161120 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4073685 161120 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4117161 161120 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
155554020 175442 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2ccc(N3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4576668 175442 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2ccc(N3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
44386772 13025 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 352 3 1 5 3.6 COc1ccc2c(c1)c1ccccc1n2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL1189868 13025 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 352 3 1 5 3.6 COc1ccc2c(c1)c1ccccc1n2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.01.071
44388987 62498 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc([N+](=O)[O-])ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178123 62498 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc([N+](=O)[O-])ccc32)cc1 10.1016/j.bmcl.2004.10.064
44397119 12411 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1185807 12411 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL433765 12411 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
4376990 193009 5 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 193009 5 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 193009 5 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
6918748 126827 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL365471 126827 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
44438726 150535 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 292 5 0 2 4.1 Cc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL395465 150535 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 292 5 0 2 4.1 Cc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
44567986 182995 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
CHEMBL479349 182995 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
155562997 175237 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL4571862 175237 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2019.111736
137643504 158409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090168 158409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
53327976 111693 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286586 111693 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
155534153 176250 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4469860 176250 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594878 176250 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
66801263 112076 0 None -40 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289970 112076 0 None -40 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
68109159 131685 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131685 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116317 131711 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 416 2 1 5 4.0 O=S(=O)(c1cncc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692930 131711 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 416 2 1 5 4.0 O=S(=O)(c1cncc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
71462331 82062 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 468 3 0 4 4.3 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165565 82062 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 468 3 0 4 4.3 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2012.06.002
24965681 84024 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207375 84024 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
137634934 155801 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1cccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4059662 155801 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1cccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
129103315 167122 0 None -3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4290311 167122 0 None -3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
137633065 156534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 6 0 6 4.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)c(Cl)n2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4068056 156534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 6 0 6 4.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)c(Cl)n2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
11849791 78040 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 262 4 2 3 1.9 NCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL209909 78040 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 262 4 2 3 1.9 NCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
2894562 154815 12 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 376 7 2 6 3.1 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
CHEMBL400349 154815 12 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 376 7 2 6 3.1 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
127046815 140023 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 518 8 0 7 4.9 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(OCc4ccccc4)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800150 140023 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 518 8 0 7 4.9 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(OCc4ccccc4)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
71463521 85301 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 217 4 1 2 2.2 CCc1[nH]c2ccncc2c1CCN(C)C 10.1007/s00044-004-0121-8
CHEMBL2260379 85301 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 217 4 1 2 2.2 CCc1[nH]c2ccncc2c1CCN(C)C 10.1007/s00044-004-0121-8
168269719 190011 0 None 2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 444 7 3 8 2.9 COc1ccccc1N1CCN(c2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5171456 190011 0 None 2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 444 7 3 8 2.9 COc1ccccc1N1CCN(c2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
57401515 68398 0 None -4466 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 498 8 0 5 4.0 COc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL1916745 68398 0 None -4466 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 498 8 0 5 4.0 COc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
145983139 165864 0 None -72 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249179 165864 0 None -72 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
90654842 112644 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
CHEMBL3233670 112644 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
CHEMBL3302936 112644 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
164614157 185153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 3 5.2 Cc1cccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4857018 185153 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 3 5.2 Cc1cccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
44446213 94928 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL254330 94928 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
16763549 117941 9 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 342 5 1 5 2.8 COCCn1c(C)c(C)c(S(=O)(=O)c2ccc(Cl)cc2)c1N 10.1016/j.bmcl.2015.03.049
CHEMBL3403344 117941 9 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 342 5 1 5 2.8 COCCn1c(C)c(C)c(S(=O)(=O)c2ccc(Cl)cc2)c1N 10.1016/j.bmcl.2015.03.049
132938109 164303 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 500 9 2 5 4.2 O=S(=O)(NC1CCN(CC(O)COc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2017.03.057
CHEMBL4212199 164303 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 500 9 2 5 4.2 O=S(=O)(NC1CCN(CC(O)COc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2017.03.057
11653679 181191 1 None -44 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 181191 1 None -44 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
139488539 171424 0 None -186 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 307 2 1 2 4.0 CCn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4462820 171424 0 None -186 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 307 2 1 2 4.0 CCn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
161 754 6 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 754 6 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 754 6 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
168292233 191860 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 4.2 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5199228 191860 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 4.2 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
145984807 165776 0 None -602 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4247275 165776 0 None -602 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
42631003 199618 13 None -10 8 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/jm5003952
CHEMBL592752 199618 13 None -10 8 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/jm5003952
58258861 127933 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 2 1 4 4.3 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664757 127933 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 2 1 4 4.3 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
89888370 129003 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 5 1 6 4.0 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669680 129003 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 5 1 6 4.0 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
11818252 175313 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.05.076
CHEMBL457351 175313 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.05.076
44388951 62529 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178234 62529 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44388956 63087 0 None 38 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178870 63087 0 None 38 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
11361090 64305 0 None 32 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181066 64305 0 None 32 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
44388950 122604 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL360234 122604 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
44389074 123312 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361572 123312 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44401277 70267 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 263 5 1 1 4.0 CNCCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL194174 70267 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 263 5 1 1 4.0 CNCCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
9867475 18013 0 None 21 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 18013 0 None 21 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
11723168 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL94422 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
11976 920 59 None -3 24 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
667467 920 59 None -3 24 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
CHEMBL908 920 59 None -3 24 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
DB01239 920 59 None -3 24 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
23815447 9844 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 8 1 6 4.1 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL114048 9844 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 8 1 6 4.1 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
146680920 171874 0 None 50 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4469309 171874 0 None 50 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
155566191 175739 0 None 13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4583082 175739 0 None 13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
90468813 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2019.06.022
CHEMBL4125735 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2019.06.022
90468813 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
CHEMBL4125735 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
90468813 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4125735 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469114 184422 0 None 257 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4846153 184422 0 None 257 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469183 185495 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4862354 185495 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469115 185842 4 None 36 17 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185842 4 None 36 17 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469187 186008 0 None 251 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 1 6 3.1 Cc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
CHEMBL4870374 186008 0 None 251 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 1 6 3.1 Cc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
164626889 186577 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 449 11 2 6 3.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4878361 186577 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 449 11 2 6 3.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
164627505 186579 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4878383 186579 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113783
162646407 179623 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4742804 179623 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
162646981 179716 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 361 3 1 7 1.2 O=S(=O)(c1cccc(F)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4743983 179716 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 361 3 1 7 1.2 O=S(=O)(c1cccc(F)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
162657990 181078 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4759927 181078 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
10115005 71684 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196466 71684 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403097 72446 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198827 72446 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10136185 127179 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365753 127179 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
9902533 133602 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133602 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10199819 133608 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371318 133608 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403103 141309 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL383373 141309 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403047 168428 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL434932 168428 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
276 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
5312149 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
CHEMBL431298 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
90468813 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4125735 161335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.bmc.2018.05.033
9824783 176603 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45977 176603 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
164618065 185352 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 408 8 1 4 3.6 O=S(=O)(c1ccccc1)N1CCc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4860124 185352 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 408 8 1 4 3.6 O=S(=O)(c1ccccc1)N1CCc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
164623617 185488 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 410 8 1 6 3.9 Cc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)o1 10.1016/j.ejmech.2021.113792
CHEMBL4862289 185488 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 410 8 1 6 3.9 Cc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)o1 10.1016/j.ejmech.2021.113792
164618728 185524 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4862752 185524 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164621287 185546 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccncc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863037 185546 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccncc3)cccc21 10.1016/j.ejmech.2021.113792
46227396 201640 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 201640 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
11818252 175313 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1021/jm8009469
CHEMBL457351 175313 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1021/jm8009469
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm8009469
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm8009469
155566665 175905 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 500 7 2 6 4.8 COc1ccc2c(c1)c(-c1[nH]c(NC(=O)Cc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4586990 175905 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 500 7 2 6 4.8 COc1ccc2c(c1)c(-c1[nH]c(NC(=O)Cc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155560943 176567 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4574931 176567 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4597364 176567 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
127047680 139917 0 None 562 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 5 1 6 4.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCNCC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799529 139917 0 None 562 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 5 1 6 4.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCNCC3)nc21 10.1016/j.bmcl.2016.04.024
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
16718922 198220 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
CHEMBL575310 198220 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
11177383 201732 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606549 201732 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11407867 201762 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
CHEMBL606704 201762 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
11223004 202214 0 None 4 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 202214 0 None 4 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
11440676 202215 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
CHEMBL609743 202215 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
11418830 202298 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.6 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)c(Cl)c1 10.1021/jm049243i
CHEMBL610257 202298 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.6 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)c(Cl)c1 10.1021/jm049243i
68115633 131718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1ccc(F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692937 131718 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1ccc(F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115804 131726 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692945 131726 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
276 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
5312149 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
CHEMBL431298 3513 50 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
25024724 62961 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785065 62961 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
25123014 200431 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 200431 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
9800707 204503 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL72574 204503 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1016/s0960-894x(00)00453-4
11723168 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
11723168 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL94422 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL94422 207494 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
16117281 60144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642880 60144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739648 60144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
23624309 176733 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460195 176733 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
68109159 131685 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131685 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115765 131731 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692950 131731 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
25024725 62962 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
CHEMBL1785066 62962 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
17940243 45470 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3cc(Br)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL152806 45470 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3cc(Br)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369828 47464 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 477 5 2 5 3.5 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154534 47464 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 477 5 2 5 3.5 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354557 47795 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154842 47795 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9803937 112364 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cccc2c(Cl)cccc12 10.1016/s0960-894x(01)00558-3
CHEMBL329482 112364 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cccc2c(Cl)cccc12 10.1016/s0960-894x(01)00558-3
10769116 158552 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 553 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2c(F)c(Br)cc(F)c2Br)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL409160 158552 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 553 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2c(F)c(Br)cc(F)c2Br)cc1N1CCN(C)CC1 10.1021/jm980532e
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
44398568 124538 2 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 1 4 2.3 NCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
CHEMBL364039 124538 2 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 1 4 2.3 NCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
9927441 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
CHEMBL93868 207394 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
10182109 71751 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 445 3 1 6 4.5 Cc1c(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.06.107
CHEMBL196644 71751 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 445 3 1 6 4.5 Cc1c(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.06.107
22557292 153572 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1ccccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL398035 153572 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1ccccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
58258866 128974 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 4 5.0 CC(C)N1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669651 128974 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 4 5.0 CC(C)N1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
7185123 10677 6 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10677 6 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44435653 147400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392976 147400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880707 8538 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1094370 8538 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10405986 18789 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1278092 18789 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44591611 184405 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL484593 184405 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
25024322 62951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 5 0 5 3.2 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785056 62951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 5 0 5 3.2 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
44435653 147400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL392976 147400 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162674129 183213 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4795995 183213 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
24965329 84037 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207388 84037 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
44476607 82352 3 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172192 82352 3 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
58258828 127932 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664756 127932 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258756 127957 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127957 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
58258776 129006 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669683 129006 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44413494 139332 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2006.04.094
CHEMBL379273 139332 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2006.04.094
44435624 89103 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236541 89103 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44293023 181578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.5 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
CHEMBL47691 181578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.5 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
45484322 198805 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL583389 198805 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263314 184786 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(OCc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485147 184786 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(OCc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
56944384 112121 0 None -4 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3290014 112121 0 None -4 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
10276057 60659 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 455 8 2 3 5.7 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4c(Cl)cccc34)cc12 10.1021/jm049615n
CHEMBL176028 60659 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 455 8 2 3 5.7 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4c(Cl)cccc34)cc12 10.1021/jm049615n
68116201 131692 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1OC(F)(F)F nan
CHEMBL3692911 131692 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1OC(F)(F)F nan
57414526 131701 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692920 131701 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115693 131722 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1cccc(C(O)C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692941 131722 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1cccc(C(O)C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
44435624 89103 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236541 89103 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
25024729 62931 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 439 4 0 5 3.6 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2F)CC1 10.1021/ml100101u
CHEMBL1784912 62931 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 439 4 0 5 3.6 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2F)CC1 10.1021/ml100101u
44435643 147599 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393107 147599 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258857 128982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128982 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
53316820 60135 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642872 60135 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739605 60135 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44435643 147599 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393107 147599 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23653135 56681 3 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642412 56681 3 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
66801551 112123 0 None -16 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290016 112123 0 None -16 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68115817 131741 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(CO)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692960 131741 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(CO)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
16019292 10993 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10993 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16118796 60098 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642853 60098 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739217 60098 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
66803595 159728 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4104622 159728 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
164622837 185898 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 479 12 2 7 3.6 COc1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
CHEMBL4868597 185898 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 479 12 2 7 3.6 COc1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
164629021 186303 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 568 12 2 7 6.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4874513 186303 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 568 12 2 7 6.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
46880655 5552 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1076684 5552 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
164622459 186101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4871678 186101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
25263342 184149 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(COc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482937 184149 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(COc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
10180527 63885 5 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL180425 63885 5 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
21071390 1987 53 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
8689 1987 53 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
CHEMBL3286580 1987 53 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
DB11957 1987 53 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
25123013 200458 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 200458 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
67085396 127935 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 434 2 1 4 4.7 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664759 127935 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 434 2 1 4 4.7 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258754 128969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
11545169 147651 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393158 147651 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44293077 187819 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 3.8 O=S(=O)(c1ccc(F)cc1F)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL49598 187819 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 3.8 O=S(=O)(c1ccc(F)cc1F)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
10113909 186075 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4871357 186075 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
25122652 200662 0 None 134 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 200662 0 None 134 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
71456942 82049 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2F)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165552 82049 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2F)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
11545169 147651 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393158 147651 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
52913106 127908 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664732 127908 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258754 128969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
58258841 129011 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669688 129011 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
9929665 66791 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL185958 66791 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
44435628 148502 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393830 148502 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
52913108 70761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
16222869 82041 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 452 4 0 5 4.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165544 82041 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 452 4 0 5 4.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435628 148502 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL393830 148502 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
118712408 114173 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 351 3 1 3 4.1 O=S(=O)(c1ccccc1)c1ccc(C2CCNCC2)c2ccccc12 10.1021/jm5003952
CHEMBL3329443 114173 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 351 3 1 3 4.1 O=S(=O)(c1ccccc1)c1ccc(C2CCNCC2)c2ccccc12 10.1021/jm5003952
52913218 70762 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950763 70762 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
9841434 11749 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1181599 11749 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL183757 11749 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
4106 2502 22 None -7 34 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2502 22 None -7 34 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2502 22 None -7 34 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2502 22 None -7 34 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
44435639 88548 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235306 88548 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16750338 62629 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783607 62629 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
71502676 118257 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 8 0 7 5.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc5ccoc5c4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409255 118257 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 8 0 7 5.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc5ccoc5c4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
134130753 142221 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(F)ccc1F 10.1016/j.ejmech.2016.09.008
CHEMBL3884325 142221 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(F)ccc1F 10.1016/j.ejmech.2016.09.008
44435639 88548 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235306 88548 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44248103 62954 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1021/ml100101u
CHEMBL1785059 62954 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1021/ml100101u
44435647 88509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL235117 88509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162659494 181354 0 None -11 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4763085 181354 0 None -11 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
58258811 127959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
44435647 88509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235117 88509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45487129 197806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL572092 197806 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
10297610 61046 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 10 2 3 5.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL176292 61046 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 10 2 3 5.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
18354552 46701 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL153918 46701 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354572 48210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3cc(C)c(C(F)(F)F)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155234 48210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3cc(C)c(C(F)(F)F)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369364 49622 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 445 6 2 6 2.9 COc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL156610 49622 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 445 6 2 6 2.9 COc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
17940121 50412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cc(I)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157285 50412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cc(I)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9825329 107449 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 456 4 2 6 4.2 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)oc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL318262 107449 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 456 4 2 6 4.2 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)oc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
18354590 119998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL350022 119998 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10286610 120864 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm050247c
CHEMBL355905 120864 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm050247c
134136921 142541 0 None 501 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3890882 142541 0 None 501 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
162650362 180013 0 None -19 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4747225 180013 0 None -19 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
46890219 6912 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 403 4 1 3 4.2 CC(C)(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084359 6912 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 403 4 1 3 4.2 CC(C)(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889894 7094 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 4 1 5 2.3 CS(=O)(=O)c1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085115 7094 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 4 1 5 2.3 CS(=O)(=O)c1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
46890265 7423 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 1 4 2.2 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(N)(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1086572 7423 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 1 4 2.2 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(N)(=O)=O 10.1016/j.bmcl.2010.03.110
44441240 93714 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 404 3 1 4 3.7 CC1(C)CN(S(=O)(=O)c2ccccc2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL247121 93714 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 404 3 1 4 3.7 CC1(C)CN(S(=O)(=O)c2ccccc2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
44441239 149917 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 3 1 5 2.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL394949 149917 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 3 1 5 2.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
10252272 142345 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 432 4 1 4 4.9 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)s3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL388674 142345 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 432 4 1 4 4.9 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)s3)cc2CC1 10.1016/j.bmcl.2006.10.036
168298632 192729 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysisDisplacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysis
ChEMBL 447 5 2 5 3.3 O=C(N[C@@H]1CCNC1)c1ccn(S(=O)(=O)c2cccc(Cl)c2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2021.128275
CHEMBL5220242 192729 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysisDisplacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysis
ChEMBL 447 5 2 5 3.3 O=C(N[C@@H]1CCNC1)c1ccn(S(=O)(=O)c2cccc(Cl)c2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2021.128275
16118928 60155 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642859 60155 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739697 60155 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
56944954 157566 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 445 7 3 4 4.0 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4080399 157566 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 445 7 3 4 4.0 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
155534201 171910 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4469870 171910 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
137645924 157549 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
CHEMBL4080312 157549 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
118654517 190064 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5172390 190064 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
145958161 162087 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4160888 162087 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137643783 158434 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090395 158434 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
164623135 185547 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863079 185547 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113792
23655466 150147 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 368 4 1 4 3.7 NCCc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL395145 150147 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 368 4 1 4 3.7 NCCc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1021/jm070521y
11559090 155561 0 None 60 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL404352 155561 0 None 60 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
23652861 56691 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 489 5 0 5 4.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642422 56691 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 489 5 0 5 4.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
7184886 10606 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10606 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53317295 56700 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642431 56700 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
24966378 84031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207382 84031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
23652994 56695 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 445 5 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642426 56695 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 445 5 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
162669595 182744 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4790020 182744 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
12051079 61365 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 4 1 3 4.1 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN 10.1016/j.bmcl.2004.01.071
CHEMBL176838 61365 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 4 1 3 4.1 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN 10.1016/j.bmcl.2004.01.071
11820174 204876 12 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 202 3 1 1 2.6 Cc1[nH]c2ccccc2c1CCN(C)C 10.1021/jm990550b
CHEMBL7580 204876 12 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 202 3 1 1 2.6 Cc1[nH]c2ccccc2c1CCN(C)C 10.1021/jm990550b
66801052 158958 0 None -69 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4095979 158958 0 None -69 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
54580137 62541 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782366 62541 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
10873805 204694 2 None -83 5 Human 6.5 pKi = 6.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(I)cc2)CC1 10.1021/jm0200411
CHEMBL73979 204694 2 None -83 5 Human 6.5 pKi = 6.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(I)cc2)CC1 10.1021/jm0200411
10991109 205167 1 None -316 5 Human 5.5 pKi = 5.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 329 5 0 2 4.1 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/jm0200411
CHEMBL78218 205167 1 None -316 5 Human 5.5 pKi = 5.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 329 5 0 2 4.1 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/jm0200411
155539483 172862 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL4515160 172862 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
71574302 86264 0 None -27 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312637 86264 0 None -27 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
156013612 177228 0 None -30 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 452 9 0 7 5.9 c1ccc2oc(SCCCCCCN3CCN(c4nsc5ccccc45)CC3)nc2c1 10.1016/j.bmc.2020.115459
CHEMBL4635603 177228 0 None -30 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 452 9 0 7 5.9 c1ccc2oc(SCCCCCCN3CCN(c4nsc5ccccc45)CC3)nc2c1 10.1016/j.bmc.2020.115459
138691317 171537 0 None -5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 211 2 1 2 3.1 CCn1cncc1-c1c[nH]c2ccccc12 10.1016/j.ejmech.2019.03.017
CHEMBL4464377 171537 0 None -5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 211 2 1 2 3.1 CCn1cncc1-c1c[nH]c2ccccc12 10.1016/j.ejmech.2019.03.017
168292270 191888 3 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 5 1 5 4.8 COc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5199814 191888 3 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 5 1 5 4.8 COc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
156010319 177042 0 None -54 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4632519 177042 0 None -54 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115459
155530553 171532 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 3 4.8 Cn1cc(CCNCc2ccc(-c3ccccc3)o2)c2ccccc21 10.1016/j.ejmech.2019.111857
CHEMBL4464285 171532 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 3 4.8 Cn1cc(CCNCc2ccc(-c3ccccc3)o2)c2ccccc21 10.1016/j.ejmech.2019.111857
118464420 138245 0 None -512 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 138245 0 None -512 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
11560362 155447 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 1 1 2 4.8 CC1(c2ccc(Br)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL403843 155447 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 1 1 2 4.8 CC1(c2ccc(Br)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
137640705 157098 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 290 3 1 7 0.9 CN1CCN(c2nc(N)nc(Cc3cccs3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4074481 157098 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 290 3 1 7 0.9 CN1CCN(c2nc(N)nc(Cc3cccs3)n2)CC1 10.1016/j.ejmech.2017.04.033
16573 177619 34 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177619 34 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
122179556 121488 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 10.6019/CHEMBL5212743
CHEMBL3582461 121488 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 10.6019/CHEMBL5212743
68115781 132260 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 3 2 5 2.0 NC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696973 132260 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 3 2 5 2.0 NC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
57392825 68397 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL1916744 68397 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233402 68397 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
137655411 158756 0 None -10 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4093971 158756 0 None -10 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
44388953 123689 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL362177 123689 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2004.10.064
16118927 60133 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642871 60133 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739586 60133 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
16718921 182660 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 O=S(=O)(Nc1ccc2c(c1)C(CCN1CCCCC1)=CC2)c1c(Cl)nc2sccn12 10.1021/jm8009469
CHEMBL478895 182660 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 O=S(=O)(Nc1ccc2c(c1)C(CCN1CCCCC1)=CC2)c1c(Cl)nc2sccn12 10.1021/jm8009469
155562423 175225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4571469 175225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
23655664 171377 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 374 4 1 5 3.7 NCCc1cn(S(=O)(=O)c2cc(Cl)c(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL446194 171377 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 374 4 1 5 3.7 NCCc1cn(S(=O)(=O)c2cc(Cl)c(Cl)s2)c2ccccc12 10.1021/jm070521y
24784323 176983 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 377 3 1 6 2.7 O=S(=O)(c1cccc(Cl)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL462529 176983 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 377 3 1 6 2.7 O=S(=O)(c1cccc(Cl)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
155543869 175010 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4566992 175010 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
57398615 71549 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71549 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71549 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68109540 131649 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692869 131649 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
137661837 159223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4098815 159223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
11271219 129627 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 463 6 1 7 4.3 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367305 129627 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 463 6 1 7 4.3 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
58158709 139159 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787246 139159 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
17940055 51295 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 417 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(F)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL158094 51295 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 417 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(F)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328649 207654 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@@H](C)NC[C@@H]4C)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95285 207654 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@@H](C)NC[C@@H]4C)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918748 126827 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1021/jm050247c
CHEMBL365471 126827 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1021/jm050247c
46890263 6687 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 451 5 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2010.03.110
CHEMBL1083481 6687 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 451 5 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2010.03.110
46890292 7260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 423 4 0 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CCCS1(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1085879 7260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 423 4 0 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CCCS1(=O)=O 10.1016/j.bmcl.2010.03.110
44425717 86347 0 None -39 5 Human 7.5 pKi = 7.5 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 484 6 1 4 5.6 CC(C)Oc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231349 86347 0 None -39 5 Human 7.5 pKi = 7.5 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 484 6 1 4 5.6 CC(C)Oc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
164624246 185943 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4869411 185943 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
2853434 117931 15 None -2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 386 3 1 2 4.9 O=S(=O)(c1ccccc1)N1C=Cc2ccccc2C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403335 117931 15 None -2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 386 3 1 2 4.9 O=S(=O)(c1ccccc1)N1C=Cc2ccccc2C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
145985533 165732 0 None -309 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246202 165732 0 None -309 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
10202564 1524 14 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
3217 1524 14 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
CHEMBL362628 1524 14 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
145959790 162293 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.0 Cc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164195 162293 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.0 Cc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137657317 159628 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 3 4.2 CN1CCN(Cc2cn(Cc3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103475 159628 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 3 4.2 CN1CCN(Cc2cn(Cc3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
71458647 81413 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 434 9 1 4 4.0 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159457 81413 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 434 9 1 4 4.0 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
145984299 165752 0 None -2238 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246655 165752 0 None -2238 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
90654856 112693 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233677 112693 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304304 112693 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
71449641 81414 0 None -24 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 468 9 1 4 4.6 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159458 81414 0 None -24 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 468 9 1 4 4.6 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
6484477 174880 9 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 276 2 0 5 2.3 CCc1cc2c(N3CCN(C)CC3)nc(C)nc2s1 10.1016/j.ejmech.2019.111857
CHEMBL4563932 174880 9 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 276 2 0 5 2.3 CCc1cc2c(N3CCN(C)CC3)nc(C)nc2s1 10.1016/j.ejmech.2019.111857
11397149 56475 0 None -1000 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632223 56475 0 None -1000 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
134139144 146115 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3919497 146115 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
134147644 149637 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3947289 149637 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
22557286 93510 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 1 7 1.1 CS(=O)(=O)c1ccccc1S(=O)(=O)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246290 93510 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 1 7 1.1 CS(=O)(=O)c1ccccc1S(=O)(=O)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
11304596 56396 0 None -19952 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631542 56396 0 None -19952 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
10573876 10462 0 None -1584 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
CHEMBL116448 10462 0 None -1584 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
156016366 177639 0 None -39 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 458 10 1 6 4.0 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
CHEMBL4641296 177639 0 None -39 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 458 10 1 6 4.0 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
145974789 163052 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 3 1 5 2.3 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176229 163052 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 3 1 5 2.3 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
242 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
34 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
60795 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
CHEMBL1112 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
DB01238 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
242 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
34 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
60795 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
CHEMBL1112 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
DB01238 470 124 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
155515408 176332 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4442062 176332 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595453 176332 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
16040768 114154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 452 4 2 4 5.3 O=S(=O)(Nc1ccc2c(c1)CNCCC2)c1csc(C(F)(F)F)c1-c1ccccc1 10.1021/jm5003952
CHEMBL3329424 114154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 452 4 2 4 5.3 O=S(=O)(Nc1ccc2c(c1)CNCCC2)c1csc(C(F)(F)F)c1-c1ccccc1 10.1021/jm5003952
20722800 66934 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL186621 66934 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
20722800 66934 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL186621 66934 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
137657598 159623 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 352 3 1 6 2.1 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4103397 159623 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 352 3 1 6 2.1 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
57392615 70770 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 341 2 1 5 2.6 Cn1c2c(c3cc(S(=O)(=O)n4cccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950772 70770 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 341 2 1 5 2.6 Cn1c2c(c3cc(S(=O)(=O)n4cccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57396848 71536 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71536 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71536 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
56944668 112112 0 None -39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290005 112112 0 None -39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
16222762 82052 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 386 3 0 4 3.7 Cc1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165555 82052 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 386 3 0 4 3.7 Cc1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
16222865 82031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165535 82031 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
11729763 118524 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 434 8 0 5 4.6 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OCc3ccccc3)cc12 10.1021/jm010943m
CHEMBL341495 118524 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 434 8 0 5 4.6 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OCc3ccccc3)cc12 10.1021/jm010943m
66800965 158194 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4087852 158194 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
145955674 162431 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)nccc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166372 162431 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)nccc32)c1 10.1016/j.ejmech.2017.12.053
56595533 65647 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
CHEMBL1834237 65647 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
135458672 117933 10 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 3 2 3 4.1 Cc1ccc(S(=O)(=O)N/N=C2\CCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403337 117933 10 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 3 2 3 4.1 Cc1ccc(S(=O)(=O)N/N=C2\CCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1016/j.bmcl.2015.03.049
156017397 177697 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 420 7 1 4 5.0 CCCC(=O)Nc1ccc2c(c1)-c1c(OCC3CC3)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4642034 177697 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 420 7 1 4 5.0 CCCC(=O)Nc1ccc2c(c1)-c1c(OCC3CC3)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
168287126 191565 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 414 6 3 7 2.9 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194826 191565 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 414 6 3 7 2.9 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
44568103 184024 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 424 4 0 5 4.2 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482100 184024 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 424 4 0 5 4.2 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
127037679 136675 0 None -40 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 438 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cc(F)ccc2F)CC1 10.1039/C5MD00166H
CHEMBL3740235 136675 0 None -40 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 438 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cc(F)ccc2F)CC1 10.1039/C5MD00166H
127026133 137821 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 5.4 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759819 137821 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 5.4 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2015.11.040
71574208 86269 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312642 86269 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
137634216 156648 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 3 0 4 4.0 CN1CCN(Cc2cn(C(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4069315 156648 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 3 0 4 4.0 CN1CCN(Cc2cn(C(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
162652175 180273 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 284 3 0 2 4.8 c1ccc(Cn2ccc3ccc(-c4ccncc4)cc32)cc1 10.1016/j.ejmech.2020.112916
CHEMBL4750657 180273 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 284 3 0 2 4.8 c1ccc(Cn2ccc3ccc(-c4ccncc4)cc32)cc1 10.1016/j.ejmech.2020.112916
71449643 81438 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159481 81438 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155549315 173829 0 None -1621 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 448 9 0 6 4.1 COc1ccccc1N1CCN(CCCCCCn2c(=O)n3c4c(cccc42)CCC3)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4538667 173829 0 None -1621 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 448 9 0 6 4.1 COc1ccccc1N1CCN(CCCCCCn2c(=O)n3c4c(cccc42)CCC3)CC1 10.1016/j.bmcl.2019.06.029
156020902 178029 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 378 5 0 4 4.3 COc1cc2c3c(c1OCC1CC1)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4646861 178029 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 378 5 0 4 4.3 COc1cc2c3c(c1OCC1CC1)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL5265814 193454 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 436 7 0 5 3.8 O=C1CC2CCc3ccsc3C2=NN1CCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
44327972 207591 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL94969 207591 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1016/j.bmcl.2005.01.031
9863380 18342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 353 5 0 5 2.9 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(C#N)cc12 10.1021/jm010943m
CHEMBL127089 18342 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 353 5 0 5 2.9 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(C#N)cc12 10.1021/jm010943m
44327972 207591 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1021/jm030030n
CHEMBL94969 207591 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1021/jm030030n
100 3805 58 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3805 58 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3805 58 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3805 58 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3805 58 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
44568022 183005 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
CHEMBL479362 183005 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
44567933 188294 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1cccc(F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL500305 188294 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1cccc(F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
145955822 162675 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4170187 162675 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
616691 154355 14 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 6 2 5 2.7 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL398698 154355 14 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 6 2 5 2.7 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
44403061 127420 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 1 4 3.5 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL365993 127420 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 1 4 3.5 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44591068 190572 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518017 190572 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
5 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
5202 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
CHEMBL39 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
DB08839 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
5 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
5202 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
CHEMBL39 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
DB08839 139 72 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
118731509 118246 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 9 1 6 4.5 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409244 118246 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 9 1 6 4.5 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
66801173 112063 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 486 8 1 7 4.4 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289958 112063 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 486 8 1 7 4.4 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44435632 89469 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237179 89469 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435632 89469 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237179 89469 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
197033 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
56595280 65636 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834225 65636 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595280 65636 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834225 65636 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
56595407 65643 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
CHEMBL1834231 65643 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
4806 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
66803500 156439 0 None -131 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 459 8 3 4 4.4 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4066971 156439 0 None -131 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 459 8 3 4 4.4 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
54586020 62540 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782365 62540 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
90656175 110846 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260808 110846 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNC2 10.1016/j.bmcl.2014.03.049
66801226 112077 0 None -33 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 7 1 6 3.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289971 112077 0 None -33 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 7 1 6 3.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
9419 35922 35 None -165 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL1442422 35922 35 None -165 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
168295653 192328 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 4 1 4 5.5 Clc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5206513 192328 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 4 1 4 5.5 Clc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
155543054 173187 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 358 8 1 2 5.9 CCCN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4522432 173187 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 358 8 1 2 5.9 CCCN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
11306131 60522 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4c(N(C)C)cccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL175718 60522 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4c(N(C)C)cccc34)CC1)C(=O)OC2 10.1021/jm049615n
145986031 165822 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248544 165822 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
126720389 162121 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 337 4 1 6 2.2 COc1ccccc1Cn1c(C)nc2c(N3CCNCC3)ccnc21 10.1016/j.ejmech.2017.12.053
CHEMBL4161480 162121 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 337 4 1 6 2.2 COc1ccccc1Cn1c(C)nc2c(N3CCNCC3)ccnc21 10.1016/j.ejmech.2017.12.053
44581974 175704 0 None -64 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 175704 0 None -64 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
57403839 71546 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949967 71546 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963008 71546 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
68109250 131630 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692850 131630 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
44390054 64473 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 283 2 1 3 3.3 Nc1ccc(S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL181382 64473 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 283 2 1 3 3.3 Nc1ccc(S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
197033 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2021.128275
CHEMBL589390 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2021.128275
197033 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 199152 64 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
23900125 163384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 415 7 1 6 2.9 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL419398 163384 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 415 7 1 6 2.9 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/s0960-894x(03)00612-7
66800959 157438 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 413 6 2 3 3.7 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4078873 157438 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 413 6 2 3 3.7 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
90469184 185632 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4864338 185632 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
44403057 133423 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 4 1 4 3.8 O=S(=O)(c1ccc(I)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370508 133423 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 4 1 4 3.8 O=S(=O)(c1ccc(I)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398718 69745 0 None -6 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69745 0 None -6 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
45488152 198929 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 198929 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
155522117 176357 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4450907 176357 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4595675 176357 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
11383990 201780 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606766 201780 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
68109087 131660 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 378 2 1 5 4.0 O=S(=O)(c1ccc2c3c(oc2c1)CC1CCC3N1)n1ccc2ccccc21 nan
CHEMBL3692879 131660 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 378 2 1 5 4.0 O=S(=O)(c1ccc2c3c(oc2c1)CC1CCC3N1)n1ccc2ccccc21 nan
162656718 180958 0 None -8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
CHEMBL4758402 180958 0 None -8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
137630632 161081 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4097893 161081 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116776 161081 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
162651101 180234 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 601 15 2 6 6.1 C[C@H](NCc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4750021 180234 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 601 15 2 6 6.1 C[C@H](NCc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
3132842 162987 9 None 10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 411 9 1 4 5.4 CCC1(C)CC(CCNCc2ccc(OC)c(OC)c2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
CHEMBL4175296 162987 9 None 10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 411 9 1 4 5.4 CCC1(C)CC(CCNCc2ccc(OC)c(OC)c2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
58258803 127950 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)ccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664775 127950 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)ccn4)ccc31)C1CCC(C2)N1 nan
145983468 165436 0 None -31 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238897 165436 0 None -31 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
11609368 155259 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 2 1 3 3.4 COc1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL402810 155259 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 2 1 3 3.4 COc1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
134142907 145299 0 None -39 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3913100 145299 0 None -39 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155532544 171751 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.9 COc1ccc2[nH]cc(CC(C)NCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4467357 171751 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.9 COc1ccc2[nH]cc(CC(C)NCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
11501432 94712 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 2 1 3 4.2 CN(C)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL252902 94712 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 2 1 3 4.2 CN(C)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
155538144 172396 0 None -12 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 295 3 1 3 4.0 CCn1cncc1-c1c[nH]c2ccc(OC(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4476520 172396 0 None -12 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 295 3 1 3 4.0 CCn1cncc1-c1c[nH]c2ccc(OC(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
155561901 175756 0 None -75 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 259 3 1 3 3.2 CCn1cncc1-c1c[nH]c2ccc(OC)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4583507 175756 0 None -75 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 259 3 1 3 3.2 CCn1cncc1-c1c[nH]c2ccc(OC)c(F)c12 10.1016/j.ejmech.2019.03.017
155547436 173572 0 None -7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2019.06.029
CHEMBL4532741 173572 0 None -7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2019.06.029
145984511 165624 0 None -34 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243497 165624 0 None -34 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
137650870 157162 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 7 0 6 3.7 COc1ccc2c(c1)c(CN1CCN(CCF)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4075316 157162 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 7 0 6 3.7 COc1ccc2c(c1)c(CN1CCN(CCF)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137661730 159505 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 478 5 0 7 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)nn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4101944 159505 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 478 5 0 7 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)nn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
142601325 185869 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185869 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
58258800 127911 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 4 3.9 [C-]#[N+]c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664735 127911 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 4 3.9 [C-]#[N+]c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
44390023 11747 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1181573 11747 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL180945 11747 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
191 403 98 None -20 29 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 403 98 None -20 29 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 403 98 None -20 29 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 403 98 None -20 29 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 403 98 None -20 29 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
56945042 158041 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4085802 158041 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
52913226 70765 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C#N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950766 70765 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C#N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
45487150 197720 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL571413 197720 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
90644077 112087 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 7 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289981 112087 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 7 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
66801028 112103 0 None -9 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 8 1 6 4.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289997 112103 0 None -9 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 8 1 6 4.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
11407544 202208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 421 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3Cl)cc12 10.1021/jm049243i
CHEMBL609736 202208 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 421 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3Cl)cc12 10.1021/jm049243i
58149665 82344 3 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172183 82344 3 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
137650795 157443 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4078912 157443 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
58149672 82345 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 392 3 0 7 2.4 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccc(F)cc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172184 82345 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 392 3 0 7 2.4 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccc(F)cc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
57392612 70754 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70754 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
58258855 127947 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 414 3 1 4 4.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2-c2ccccc2)CC2CCC1N2 nan
CHEMBL3664771 127947 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 414 3 1 4 4.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2-c2ccccc2)CC2CCC1N2 nan
10111488 17998 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 398 6 0 5 3.9 COc1ccc2c(c1)c(CCN1CCCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126263 17998 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 398 6 0 5 3.9 COc1ccc2c(c1)c(CCN1CCCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
66801625 158285 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 7 2 3 5.7 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4088925 158285 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 7 2 3 5.7 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
168280347 191169 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
CHEMBL5188859 191169 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
57392612 70754 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950755 70754 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL5081379 214746 0 None -524 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
156013736 177263 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 404 6 1 4 4.2 C#CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4636165 177263 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 404 6 1 4 4.2 C#CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
90666903 109449 0 None -44 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
CHEMBL3220219 109449 0 None -44 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
164608896 184420 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 184420 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155544139 173353 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(OCc2nc(N)nc(N3CCN(C)CC3)n2)ccc1Cl 10.1016/j.ejmech.2019.06.022
CHEMBL4527124 173353 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(OCc2nc(N)nc(N3CCN(C)CC3)n2)ccc1Cl 10.1016/j.ejmech.2019.06.022
156022234 178210 0 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 380 5 1 4 4.2 CCCC(=O)Nc1ccc2c(c1)-c1c(OC)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4649697 178210 0 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 380 5 1 4 4.2 CCCC(=O)Nc1ccc2c(c1)-c1c(OC)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
57384073 77205 0 None -4466 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 COc1ccccc1N1CCN(CCCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL2079256 77205 0 None -4466 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 COc1ccccc1N1CCN(CCCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
71458652 81435 0 None -35 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159478 81435 0 None -35 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
155515324 169955 0 None 3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 382 4 1 8 0.8 CN1CCN(c2nc(N)nc(CS(=O)(=O)c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4441655 169955 0 None 3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 382 4 1 8 0.8 CN1CCN(c2nc(N)nc(CS(=O)(=O)c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
3649661 138219 7 None -489 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 138219 7 None -489 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
26987 949 33 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 33 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 33 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 33 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 33 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
137641832 158243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 327 3 1 5 2.6 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
CHEMBL4088416 158243 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 327 3 1 5 2.6 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
137651887 157299 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 7 2 3 4.6 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4077040 157299 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 7 2 3 4.6 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
145953749 162388 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 4 1 5 2.5 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4165620 162388 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 4 1 5 2.5 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
134131482 142132 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 649 13 1 7 7.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3883432 142132 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 649 13 1 7 7.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134131347 142239 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 635 12 1 7 7.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884690 142239 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 635 12 1 7 7.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
127046963 139574 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 413 5 0 7 2.7 CC(C)CS(=O)(=O)n1ccc2c(-c3cccnc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797293 139574 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 413 5 0 7 2.7 CC(C)CS(=O)(=O)n1ccc2c(-c3cccnc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
24784577 190362 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 5 0 6 4.3 CCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL517707 190362 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 5 0 6 4.3 CCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
11338273 201796 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606868 201796 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
137634321 156363 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(C(C)C)cc3)c2c1 10.1021/acs.jmedchem.6b01662
CHEMBL4066047 156363 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(C(C)C)cc3)c2c1 10.1021/acs.jmedchem.6b01662
45488165 196911 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL566218 196911 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
69485025 156025 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 505 6 0 6 4.2 CC(C)Oc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4062233 156025 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 505 6 0 6 4.2 CC(C)Oc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
25117681 200556 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599023 200556 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
66801701 159329 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 471 8 2 3 5.3 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4099997 159329 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 471 8 2 3 5.3 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
162653506 180532 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCCCC3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4753614 180532 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCCCC3)ccc21 10.1016/j.ejmech.2020.112916
145984737 165579 0 None -724 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242392 165579 0 None -724 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
135367816 164835 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164835 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
173 3262 95 None -41 23 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
5011 3262 95 None -41 23 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
CHEMBL18772 3262 95 None -41 23 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
57392612 70754 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70754 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
68639205 160967 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4099525 160967 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4115947 160967 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
145962993 161426 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4126962 161426 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
155516282 170069 0 None -20 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)cc1 10.1016/j.bmcl.2019.06.029
CHEMBL4443185 170069 0 None -20 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)cc1 10.1016/j.bmcl.2019.06.029
22028199 198335 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL576312 198335 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ncccc21 10.1016/j.bmcl.2009.10.067
164616980 185282 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 8 1 5 5.3 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4859019 185282 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 8 1 5 5.3 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
57401298 70760 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950761 70760 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 nan
58258819 127917 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5ccccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664741 127917 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5ccccc5c4)ccc31)C1CCC(C2)N1 nan
44414681 80190 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1ccc(S(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
CHEMBL213589 80190 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1ccc(S(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
155527391 171241 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4459863 171241 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
162647987 179914 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 437 4 1 7 2.9 O=S(=O)(c1cccc(F)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4746063 179914 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 437 4 1 7 2.9 O=S(=O)(c1cccc(F)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
57401298 70760 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950761 70760 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57403833 71470 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71470 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71470 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68115688 131714 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 2 1 6 3.5 Cn1ncc2cc(S(=O)(=O)c3cc(Cl)c4oc5c(c4c3)CNCC5)ccc21 nan
CHEMBL3692933 131714 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 2 1 6 3.5 Cn1ncc2cc(S(=O)(=O)c3cc(Cl)c4oc5c(c4c3)CNCC5)ccc21 nan
162674561 183271 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
CHEMBL4796647 183271 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
137648438 157879 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 483 6 0 7 3.5 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4083959 157879 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 483 6 0 7 3.5 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01662
9817950 18028 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 304 3 1 5 3.2 CN(C)CCc1cn(C(=O)OC(C)(C)C)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL126420 18028 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 304 3 1 5 3.2 CN(C)CCc1cn(C(=O)OC(C)(C)C)c2ccc(O)cc12 10.1021/jm010943m
2921525 54870 14 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL1379600 54870 14 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL1613157 54870 14 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
44476801 82349 3 None - 1 Human 6.4 pKi = 6.4 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172189 82349 3 None - 1 Human 6.4 pKi = 6.4 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
44476801 82349 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172189 82349 3 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
117209964 186134 1 None -5 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 186134 1 None -5 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118648 76321 0 None -74 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 76321 0 None -74 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
145971739 163094 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)nccc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176992 163094 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)nccc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
155519516 176358 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4447659 176358 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595677 176358 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
118731356 118192 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409039 118192 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
57395086 71553 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
CHEMBL1949966 71553 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
CHEMBL1963029 71553 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
71451456 81420 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 8 1 4 3.5 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(F)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159463 81420 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 8 1 4 3.5 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(F)c2)CC1 10.1016/j.ejmech.2012.07.043
156016485 177773 0 None -380 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 0 7 4.7 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2cccc3c2n1CCC3 10.1016/j.bmc.2020.115459
CHEMBL4642981 177773 0 None -380 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 0 7 4.7 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2cccc3c2n1CCC3 10.1016/j.bmc.2020.115459
11849203 79856 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.2 CNCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212227 79856 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.2 CNCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
15281645 168348 7 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
CHEMBL434365 168348 7 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
162673219 183144 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4795207 183144 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
118626161 165599 0 None -53 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242858 165599 0 None -53 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
162647425 179577 1 None 10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4741978 179577 1 None 10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
15281645 168348 7 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.7b00085
CHEMBL434365 168348 7 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.7b00085
57402070 71563 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71563 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71563 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
68109060 131625 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccc(Cl)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692845 131625 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccc(Cl)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
68109319 131628 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692848 131628 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
162659287 181289 0 None -34 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4762226 181289 0 None -34 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
162666577 182333 0 None -28 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4784414 182333 0 None -28 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
53327611 69754 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
162647097 179719 0 None -41 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4744007 179719 0 None -41 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
44393113 63631 0 None -190 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 358 7 3 7 3.5 CC(Nc1nc(N)nc(NCCc2cccs2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
CHEMBL180086 63631 0 None -190 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 358 7 3 7 3.5 CC(Nc1nc(N)nc(NCCc2cccs2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
155557443 174644 0 None -181 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 3 2.7 COc1ccc2[nH]cc(-c3cncn3C)c2c1F 10.1016/j.ejmech.2019.03.017
CHEMBL4558202 174644 0 None -181 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 3 2.7 COc1ccc2[nH]cc(-c3cncn3C)c2c1F 10.1016/j.ejmech.2019.03.017
137637994 155942 0 None -26 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4061131 155942 0 None -26 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
164614828 185269 0 None 3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4858771 185269 0 None 3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
168290376 191945 1 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 411 3 0 3 6.1 FC1(F)CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5200705 191945 1 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 411 3 0 3 6.1 FC1(F)CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
44582675 189701 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189701 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
137633663 156602 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 4 0 5 3.3 CC(=O)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068846 156602 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 4 0 5 3.3 CC(=O)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
57400277 71561 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949771 71561 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963078 71561 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
168287508 191531 0 None -97 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 438 9 3 8 3.1 Nc1nc(N)nc(NCCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194270 191531 0 None -97 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 438 9 3 8 3.1 Nc1nc(N)nc(NCCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
164613499 185038 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 358 8 1 3 4.4 c1ccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4855189 185038 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 358 8 1 3 4.4 c1ccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
44455426 155149 0 None -54 12 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155149 0 None -54 12 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
58258854 128971 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4ccnc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669648 128971 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4ccnc5ccccc45)ccc31)C1CCC(C2)N1 nan
134131296 142156 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 557 9 1 7 4.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3883620 142156 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 557 9 1 7 4.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
71458723 84417 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2163740 84417 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219873 84417 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
25263323 185046 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485531 185046 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25263321 184692 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485010 184692 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
44398555 68035 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 293 4 3 5 1.7 COc1cc(N)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm050247c
CHEMBL191415 68035 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 293 4 3 5 1.7 COc1cc(N)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm050247c
132495282 145777 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3916787 145777 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
46890188 7255 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 1 3 3.1 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)C(N)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1085852 7255 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 1 3 3.1 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)C(N)=O 10.1016/j.bmcl.2010.03.110
22557219 93713 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 Cc1cc(N2CC(C)NC(C)C2)c2c(c1)N(S(=O)(=O)c1ccc(Cl)cc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL247120 93713 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 Cc1cc(N2CC(C)NC(C)C2)c2c(c1)N(S(=O)(=O)c1ccc(Cl)cc1)CCO2 10.1016/j.bmcl.2006.12.093
162653427 180395 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 307 3 0 4 2.3 CN(C)c1cccc2c1ccn2S(=O)(=O)N1CCCCC1 10.1016/j.ejmech.2020.112916
CHEMBL4751913 180395 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 307 3 0 4 2.3 CN(C)c1cccc2c1ccn2S(=O)(=O)N1CCCCC1 10.1016/j.ejmech.2020.112916
145983018 165517 0 None -436 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4240910 165517 0 None -436 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
134151729 153445 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3979307 153445 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
90654854 112683 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233676 112683 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304183 112683 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL5282788 194172 0 None -6 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 422 7 0 5 3.5 O=C1CC2Cc3ccsc3C2=NN1CCCCN1CCN(Cc2ccccc2)CC1 10.1016/j.bmc.2023.117256
57400281 71552 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949965 71552 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963028 71552 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
69363431 161034 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4082073 161034 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116440 161034 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
9888211 21416 13 None -501 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21416 13 None -501 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11168182 3534 25 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3534 25 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3534 25 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
58158673 139025 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 4 2 4 1.6 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)NCC2)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785853 139025 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 4 2 4 1.6 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)NCC2)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
46880532 6300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1021/jm5003952
CHEMBL1081794 6300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1021/jm5003952
11532574 114175 11 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1021/jm5003952
CHEMBL3329445 114175 11 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1021/jm5003952
44389099 64837 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182000 64837 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
9927441 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL93868 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
23501288 193043 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5205533 193043 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5222932 193043 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
2726 919 68 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
621 919 68 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
83 919 68 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
CHEMBL71 919 68 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
DB00477 919 68 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
135398737 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
11532574 114175 11 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of LSD from recombinant human 5-HT6R assessed as inhibition constantDisplacement of LSD from recombinant human 5-HT6R assessed as inhibition constant
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1016/j.bmcl.2021.128275
CHEMBL3329445 114175 11 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of LSD from recombinant human 5-HT6R assessed as inhibition constantDisplacement of LSD from recombinant human 5-HT6R assessed as inhibition constant
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1016/j.bmcl.2021.128275
137633827 156603 0 None 1071 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 377 3 1 5 3.8 O=S(=O)(c1cccc2ccccc12)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
CHEMBL4068850 156603 0 None 1071 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 377 3 1 5 3.8 O=S(=O)(c1cccc2ccccc12)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
135398737 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
38 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
722 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
CHEMBL42 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
DB00363 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
155514378 169850 0 None 75 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cccc2ncccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4440130 169850 0 None 75 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cccc2ncccc12 10.1021/acsmedchemlett.6b00056
135398737 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
38 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
722 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
CHEMBL42 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
DB00363 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
53322547 56685 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
CHEMBL1642416 56685 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
135398737 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
38 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
722 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
CHEMBL42 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
DB00363 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
90469117 184906 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1cc(F)ccc1F)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4853195 184906 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1cc(F)ccc1F)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
134131307 142173 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 10 0 6 4.9 CN(CCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3883921 142173 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 10 0 6 4.9 CN(CCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
137630453 161063 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4093699 161063 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116631 161063 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
44403092 70634 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL195018 70634 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403084 71744 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196622 71744 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403044 161711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL413525 161711 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
46880532 6300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081794 6300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
164612125 184656 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.1 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4849702 184656 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.1 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113792
135398737 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
38 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
722 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
CHEMBL42 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
DB00363 958 93 None -4 89 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
155535879 176669 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4472629 176669 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4598209 176669 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
127046982 139640 0 None 93 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797717 139640 0 None 93 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
49836615 18788 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1278091 18788 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
44591592 184136 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL482757 184136 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
57396813 71545 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
10205655 60551 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL175884 60551 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
11383202 201761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1 10.1021/jm049243i
CHEMBL606703 201761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1 10.1021/jm049243i
11210467 202209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
CHEMBL609737 202209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
11406161 202210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1F 10.1021/jm049243i
CHEMBL609738 202210 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1F 10.1021/jm049243i
11245641 202212 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 3 3 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
CHEMBL609740 202212 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 3 3 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
11452988 202240 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
CHEMBL609991 202240 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
68109120 131679 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 4 4.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CF)NCC3 nan
CHEMBL3692898 131679 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 4 4.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CF)NCC3 nan
68115669 131717 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1ccc(F)c(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692936 131717 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1ccc(F)c(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58258848 127929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4cc(Cl)c5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664753 127929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4cc(Cl)c5ccccc54)ccc31)C1CCC(C2)N1 nan
9927441 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
9927441 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL93868 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL93868 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
9927441 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL93868 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
56593798 65688 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834342 65688 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
52913102 70756 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950757 70756 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
9927441 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL93868 207394 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
56944383 112119 0 None -9 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112119 0 None -9 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
4106 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
44474797 14064 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL1197505 14064 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574625 14064 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
4106 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2502 22 None -2 34 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
25024731 62968 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 505 4 0 5 5.0 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 10.1021/ml100101u
CHEMBL1785072 62968 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 505 4 0 5 5.0 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 10.1021/ml100101u
44435620 148994 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL394231 148994 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162649235 180074 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4747978 180074 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
52913102 70756 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950757 70756 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 nan
16116899 60100 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642846 60100 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739232 60100 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
44435620 148994 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394231 148994 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45484381 198489 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
CHEMBL577687 198489 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
68115746 132248 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 5 2.8 N#Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696961 132248 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 5 2.8 N#Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
16222545 82034 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165538 82034 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
44435612 88796 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236405 88796 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
25122651 200249 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 200249 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
58258811 127959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127959 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
16070169 60095 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642850 60095 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739214 60095 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
131999484 182603 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182603 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182603 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
10023874 159363 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.6b01662
CHEMBL4100411 159363 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.6b01662
44435612 88796 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236405 88796 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
71455149 82045 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Br)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165548 82045 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Br)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
45484398 196867 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565977 196867 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263340 184170 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 368 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(F)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
CHEMBL482990 184170 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 368 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(F)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
10112811 166300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL427134 166300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
68109102 131666 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692885 131666 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
68109495 131672 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CCO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692891 131672 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CCO)c2oc3c(c2c1)CNCC3 nan
44435642 88637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL235734 88637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258759 127967 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 5 4.9 CC(C)n1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664792 127967 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 5 4.9 CC(C)n1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
44435642 88637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235734 88637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
53327611 69754 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
68115612 131700 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cccc(CO)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692919 131700 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cccc(CO)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25067564 201300 0 None 61 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 201300 0 None 61 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
52913108 70761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70761 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
58258862 127952 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cc[nH]c45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664777 127952 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cc[nH]c45)ccc31)C1CCC(C2)N1 nan
16112801 181091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
CHEMBL476006 181091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
137628805 160988 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4077537 160988 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4116136 160988 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
16112801 181091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL476006 181091 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
10159058 130183 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL367867 130183 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
68115740 132262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cc[nH]n2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696975 132262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cc[nH]n2)c2oc3c(c2c1)CNCC3 nan
25122653 200527 0 None 17 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 200527 0 None 17 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
16222870 82024 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 400 4 0 5 4.0 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165528 82024 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 400 4 0 5 4.0 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435635 89202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236772 89202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
57399549 70755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 nan
CHEMBL1950756 70755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 nan
58258853 128998 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669675 128998 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
44403055 69847 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193824 69847 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435635 89202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236772 89202 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880709 7447 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
CHEMBL1086720 7447 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
57399549 70755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950756 70755 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44554393 18547 0 None 61 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18547 0 None 61 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
49836823 18710 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
CHEMBL1277466 18710 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
155548127 173775 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 2.9 CCCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4537294 173775 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 2.9 CCCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
44435641 147597 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393106 147597 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5084167 214899 0 None -19 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.1c00497
162647173 179631 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
CHEMBL4742856 179631 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
162643494 181649 0 None -3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4775997 181649 0 None -3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
71458812 82047 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Cl)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165550 82047 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Cl)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
58258811 127959 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127959 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
58258753 129004 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669681 129004 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
44435641 147597 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393106 147597 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880608 6020 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080316 6020 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
44292800 176697 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 446 3 1 5 4.5 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3(O)CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45987 176697 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 446 3 1 5 4.5 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3(O)CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
45484382 196817 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
CHEMBL565730 196817 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
45484297 197296 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568672 197296 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
10112809 123140 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 4 2 3 4.9 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1021/jm049615n
CHEMBL361230 123140 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 4 2 3 4.9 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1021/jm049615n
57392613 70758 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 nan
CHEMBL1950759 70758 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 nan
52913100 127907 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 1 5 3.4 CN(C)Cc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
CHEMBL3664731 127907 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 1 5 3.4 CN(C)Cc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
58258836 127943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258857 128982 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128982 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
135398737 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
38 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
722 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
CHEMBL42 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
DB00363 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
10337743 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
8429 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
CHEMBL571858 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
53323439 60157 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642873 60157 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739699 60157 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
54752954 138950 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785100 138950 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
57392613 70758 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950759 70758 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164610173 184998 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 412 8 1 5 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCCC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4854460 184998 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 412 8 1 5 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCCC3)cccc21 10.1016/j.ejmech.2021.113792
10337743 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
155542160 173114 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4520580 173114 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
10337743 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
8429 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
CHEMBL571858 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
24967099 84036 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207387 84036 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
44435627 88500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235070 88500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
58258768 127937 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 2 2 5 3.3 Cc1cc(S(=O)(=O)c2ccc(N)cc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664761 127937 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 2 2 5 3.3 Cc1cc(S(=O)(=O)c2ccc(N)cc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258772 127944 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127944 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44435627 88500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235070 88500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
9866222 101727 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 409 3 0 5 3.9 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
CHEMBL299569 101727 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 409 3 0 5 3.9 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
10337743 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
8429 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
CHEMBL571858 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
49836621 18655 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276926 18655 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
68108527 131688 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 293 3 1 3 3.7 COc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692907 131688 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 293 3 1 3 3.7 COc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
57414528 131702 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1ccc(OC(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692921 131702 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1ccc(OC(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
10131565 117103 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 330 5 1 5 2.4 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL339337 117103 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 330 5 1 5 2.4 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
135 2532 43 None -21 58 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2532 43 None -21 58 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2532 43 None -21 58 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2532 43 None -21 58 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2532 43 None -21 58 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
145983961 165425 0 None -44 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238679 165425 0 None -44 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
145985692 165444 0 None -131 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239091 165444 0 None -131 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
44403062 71993 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 5 1 5 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL197397 71993 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 5 1 5 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
57393363 71564 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71564 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71564 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
66800939 112058 0 None -26 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289953 112058 0 None -26 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
66801062 112118 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290011 112118 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
68109432 131629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 328 2 2 5 2.5 Nc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692849 131629 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 328 2 2 5 2.5 Nc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
10202396 60481 3 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL175471 60481 3 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL5077293 214491 0 None -141 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
1574 81 60 None 1 21 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
218 81 60 None 1 21 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
CHEMBL266591 81 60 None 1 21 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
22857296 29150 0 None -61 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 29150 0 None -61 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
9856041 24114 3 None -109 8 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 24114 3 None -109 8 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
11849201 78035 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccccc1N1CCNCC1 10.1021/jm060469q
CHEMBL209893 78035 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccccc1N1CCNCC1 10.1021/jm060469q
132503215 157750 0 None -10 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4082456 157750 0 None -10 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
44443506 94066 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 7 1 5 4.2 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL248994 94066 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 7 1 5 4.2 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
162657904 181113 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCCCC3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4760297 181113 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCCCC3)cc21 10.1016/j.ejmech.2020.112916
168278234 191081 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 365 5 1 4 4.3 CN(CCO)c1nc2ccccc2c2c1ccn2Cc1cccc(Cl)c1 10.1016/j.ejmech.2022.114329
CHEMBL5187539 191081 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 365 5 1 4 4.3 CN(CCO)c1nc2ccccc2c2c1ccn2Cc1cccc(Cl)c1 10.1016/j.ejmech.2022.114329
6758 167116 75 None - 1 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
CHEMBL429023 167116 75 None - 1 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
168288780 191448 0 None -23 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5193103 191448 0 None -23 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
4397947 179599 6 None 1 2 Human 4.4 pKi = 4.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 323 3 0 3 2.5 CN(C)CCN1C(=O)c2ccccc2N(C)C(=O)c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4742201 179599 6 None 1 2 Human 4.4 pKi = 4.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 323 3 0 3 2.5 CN(C)CCN1C(=O)c2ccccc2N(C)C(=O)c2ccccc21 10.1016/j.bmcl.2020.127493
118736376 118948 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423340 118948 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
162653726 180541 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 272 2 0 4 2.5 CS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4753752 180541 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 272 2 0 4 2.5 CS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
9885982 104184 0 None -1348 2 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptorCompound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 375 3 0 3 4.0 Brc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
CHEMBL309750 104184 0 None -1348 2 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptorCompound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 375 3 0 3 4.0 Brc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
155551353 173962 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 323 1 1 2 3.2 Cn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4541526 173962 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 323 1 1 2 3.2 Cn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
162662150 181394 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccncc3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4763536 181394 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccncc3)ccc21 10.1016/j.ejmech.2020.112916
11522477 94064 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL248985 94064 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
44567983 179106 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL471783 179106 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
162656454 180968 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 449 5 1 8 2.8 COc1cccc(S(=O)(=O)n2c(-c3ccccc3)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4758494 180968 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 449 5 1 8 2.8 COc1cccc(S(=O)(=O)n2c(-c3ccccc3)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
71463517 85297 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 287 2 1 5 2.2 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260375 85297 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 287 2 1 5 2.2 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccncc12 10.1007/s00044-004-0121-8
57391729 69746 0 None -5 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69746 0 None -5 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
24784066 176189 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 343 3 1 6 2.1 O=S(=O)(c1ccccc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459349 176189 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 343 3 1 6 2.1 O=S(=O)(c1ccccc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
16222759 82027 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165531 82027 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
11257897 131370 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm049615n
CHEMBL368871 131370 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm049615n
44403080 71422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
CHEMBL195987 71422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
52912979 127902 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127902 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
71454997 81411 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 490 9 1 5 5.1 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159455 81411 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 490 9 1 5 5.1 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
156015194 177553 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 377 4 2 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640332 177553 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 377 4 2 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
24893978 1010 9 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 1010 9 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 1010 9 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
90656161 110832 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cncc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260793 110832 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cncc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
164611003 185344 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 185344 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
3005573 57440 50 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
CHEMBL1655 57440 50 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
134156520 154115 0 None -93 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 501 13 1 5 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3985152 154115 0 None -93 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 501 13 1 5 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
90654831 109826 0 None -758 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 CCOc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233401 109826 0 None -758 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 CCOc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
4011 82408 49 None -28 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 82408 49 None -28 24 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
168269921 190080 0 None -1380 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 430 8 0 7 3.4 O=c1n(CCCCCCN2CCN(c3cccc4cccnc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5172673 190080 0 None -1380 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 430 8 0 7 3.4 O=c1n(CCCCCCN2CCN(c3cccc4cccnc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
156013588 177201 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 353 3 2 4 2.9 COc1cc2c3c(c1OC)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4635229 177201 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 353 3 2 4 2.9 COc1cc2c3c(c1OC)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
124247485 164069 8 None -4 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 164069 8 None -4 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
138691329 170723 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(Cl)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4452121 170723 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(Cl)cc12 10.1016/j.ejmech.2019.03.017
155551197 173956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 382 6 2 2 6.4 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)s3)cccc2c1 10.1016/j.ejmech.2019.111857
CHEMBL4541384 173956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 382 6 2 2 6.4 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)s3)cccc2c1 10.1016/j.ejmech.2019.111857
155557661 174650 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 306 6 2 3 4.4 c1coc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4558397 174650 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 306 6 2 3 4.4 c1coc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
44395633 66268 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 362 5 0 4 3.7 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL184671 66268 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 362 5 0 4 3.7 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
145957184 162081 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 5 1 5 3.3 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4160798 162081 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 5 1 5 3.3 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
126720444 162750 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 6 1 5 4.1 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4171504 162750 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 6 1 5 4.1 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C)c1 10.1016/j.ejmech.2017.12.053
45487100 197803 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 381 4 1 8 2.2 NCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL572087 197803 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 381 4 1 8 2.2 NCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2ncccc21 10.1016/j.bmcl.2009.10.067
155554955 174320 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.1 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4550561 174320 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.1 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
25263317 174440 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 317 4 1 2 4.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL455332 174440 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 317 4 1 2 4.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
66801230 112056 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 436 8 1 7 3.2 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289951 112056 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 436 8 1 7 3.2 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
44459048 90981 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 356 4 3 5 2.3 CNc1cc(S(=O)(=O)Nc2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
CHEMBL23965 90981 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 356 4 3 5 2.3 CNc1cc(S(=O)(=O)Nc2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
44401620 68639 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 241 2 1 2 4.0 Nc1ccc(SC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL191844 68639 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 241 2 1 2 4.0 Nc1ccc(SC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
155568246 176100 0 None -186 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 528 9 2 5 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(OC)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4591440 176100 0 None -186 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 528 9 2 5 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(OC)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
145962006 161572 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4129055 161572 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
23786472 9541 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 434 8 0 5 4.6 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
CHEMBL112285 9541 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 434 8 0 5 4.6 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
44403052 69818 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 4 1 4 3.9 O=S(=O)(c1ccccc1Br)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193657 69818 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 4 1 4 3.9 O=S(=O)(c1ccccc1Br)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
68108593 131624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692844 131624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
16222764 82028 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165532 82028 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL5093017 215401 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc(F)c(Cl)c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
66800942 112045 0 None -112 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 416 6 1 6 2.7 Cc1cccc(S(=O)(=O)NCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289708 112045 0 None -112 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 416 6 1 6 2.7 Cc1cccc(S(=O)(=O)NCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
10994400 205121 0 None -467 4 Human 6.4 pKi = 6.4 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
CHEMBL77855 205121 0 None -467 4 Human 6.4 pKi = 6.4 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
164619216 185664 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185664 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
58258845 127948 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 4 2 5 2.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2CCO)CC2CCC1N2 nan
CHEMBL3664772 127948 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 4 2 5 2.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2CCO)CC2CCC1N2 nan
155511929 176277 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4436319 176277 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595069 176277 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
134155645 151073 0 None -30 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3958956 151073 0 None -30 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
24861250 200000 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cellsInhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cells
ChEMBL 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 10.1016/j.bmc.2009.09.023
CHEMBL595252 200000 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cellsInhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cells
ChEMBL 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 10.1016/j.bmc.2009.09.023
155522218 170637 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
CHEMBL4451231 170637 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
90654838 112687 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233668 112687 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304237 112687 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
52912981 127903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
CHEMBL3664728 127903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
58258823 127923 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cncc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664747 127923 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cncc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258842 128990 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 412 5 2 6 2.7 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCCO)c31)C1CCC(C2)N1 nan
CHEMBL3669667 128990 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 412 5 2 6 2.7 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCCO)c31)C1CCC(C2)N1 nan
44395663 122928 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
CHEMBL360642 122928 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
10156876 18826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 6 0 5 3.5 COc1ccc2c(c1)c(CCN1CCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL127975 18826 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 6 0 5 3.5 COc1ccc2c(c1)c(CCN1CCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44438729 93855 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 293 5 1 3 3.4 CN(C)CCc1cn(Cc2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247885 93855 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 293 5 1 3 3.4 CN(C)CCc1cn(Cc2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
53319475 60130 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642868 60130 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739583 60130 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16118926 60153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642857 60153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739695 60153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
118654518 191526 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5194172 191526 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
10182052 135190 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 3 1 5 5.5 Cc1c(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL372033 135190 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 3 1 5 5.5 Cc1c(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
155526468 171214 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4459485 171214 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
66801251 112120 0 None -16 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 507 7 1 6 5.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3290013 112120 0 None -16 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 507 7 1 6 5.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68115866 132245 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1ccc(F)cc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696958 132245 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1ccc(F)cc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL5077178 214487 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)cc1 10.1021/acs.jmedchem.1c00497
CHEMBL5093250 215420 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)c(F)c1 10.1021/acs.jmedchem.1c00497
44403071 140789 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1cccc(C(F)(F)F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL381871 140789 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1cccc(C(F)(F)F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
274 3339 44 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
5312145 3339 44 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
CHEMBL433461 3339 44 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
134138168 147691 0 None -39 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147691 0 None -39 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44438716 93852 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 364 11 0 4 4.3 CCCCCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL247871 93852 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 364 11 0 4 4.3 CCCCCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
137655929 158948 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
CHEMBL4095896 158948 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
155552356 174075 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4544262 174075 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
44438731 93856 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 0 2 4.8 CN(C)CCc1cn(Cc2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247886 93856 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 0 2 4.8 CN(C)CCc1cn(Cc2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
137650705 157234 0 None -12 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076408 157234 0 None -12 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
19958507 99421 0 None -891 5 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL282829 99421 0 None -891 5 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
49780170 17179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256251 17179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
118736373 118945 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 545 7 0 9 3.6 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423337 118945 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 545 7 0 9 3.6 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
44401550 69815 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.6 Nc1ccc(CC2C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL193637 69815 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.6 Nc1ccc(CC2C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
136152964 194939 0 None -1548 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 194939 0 None -1548 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
5206725 154080 13 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 402 6 1 5 4.5 CN1CCN(c2ccc([N+](=O)[O-])c(NC(c3ccccc3)c3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL398481 154080 13 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 402 6 1 5 4.5 CN1CCN(c2ccc([N+](=O)[O-])c(NC(c3ccccc3)c3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12017574 204799 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc(Cl)cc3)c12 10.1016/s0960-894x(00)00453-4
CHEMBL75029 204799 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc(Cl)cc3)c12 10.1016/s0960-894x(00)00453-4
9907512 18696 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/jm010943m
CHEMBL127732 18696 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/jm010943m
145985823 165924 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250475 165924 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
145963274 161582 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4129259 161582 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
45484352 198636 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL579063 198636 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
45484339 198903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 389 5 0 5 3.6 O=S(=O)(c1cccc(Cl)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
CHEMBL584474 198903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 389 5 0 5 3.6 O=S(=O)(c1cccc(Cl)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
155562755 175203 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4571059 175203 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
71151767 118241 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4F)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409239 118241 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4F)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118736374 118946 0 None -5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 559 8 0 9 4.0 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423338 118946 0 None -5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 559 8 0 9 4.0 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
66801605 112065 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 520 8 1 7 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289960 112065 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 520 8 1 7 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68115766 131737 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)C(=O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692956 131737 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)C(=O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
25263311 184649 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484964 184649 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
125513586 162877 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)nccc32)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4173336 162877 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)nccc32)cc1 10.1016/j.ejmech.2017.12.053
11232643 133473 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1cn2c3c(cccc13)-c1ccccc1S2(=O)=O 10.1016/j.bmcl.2006.08.068
CHEMBL3706857 133473 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1cn2c3c(cccc13)-c1ccccc1S2(=O)=O 10.1016/j.bmcl.2006.08.068
155535154 172042 0 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 556 9 1 7 5.2 COc1ccc(-c2c3n(c(=O)n(CCCCN4CCCC(c5c[nH]c6ccc(OC)cc56)C4)c2=O)CCCC3)cc1 10.1016/j.ejmech.2019.07.027
CHEMBL4471755 172042 0 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 556 9 1 7 5.2 COc1ccc(-c2c3n(c(=O)n(CCCCN4CCCC(c5c[nH]c6ccc(OC)cc56)C4)c2=O)CCCC3)cc1 10.1016/j.ejmech.2019.07.027
52912979 127902 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127902 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
71574306 86266 0 None -26 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
CHEMBL2312639 86266 0 None -26 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
155557500 174646 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4558215 174646 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
145985224 165488 0 None -114 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240162 165488 0 None -114 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
145972025 164479 0 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 409 4 1 3 4.1 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4214208 164479 0 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 409 4 1 3 4.1 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168284840 191296 0 None -147 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 439 5 0 6 3.8 O=c1n(CC2CCC(CN3CCN(c4cccc(Cl)c4)CC3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5190996 191296 0 None -147 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 439 5 0 6 3.8 O=c1n(CC2CCC(CN3CCN(c4cccc(Cl)c4)CC3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
57399093 68439 0 None -138 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 443 9 0 4 4.9 CCN(CCCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
CHEMBL1917360 68439 0 None -138 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 443 9 0 4 4.9 CCN(CCCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
52912977 127901 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127901 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
44397550 71192 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL188285 71192 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL195621 71192 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
44395632 122350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL359967 122350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2004.09.003
1574 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
218 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
CHEMBL266591 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
20901207 10984 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10984 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
1574 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
218 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
CHEMBL266591 81 60 None 1 21 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
44568020 183935 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL481472 183935 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
56944955 159691 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4104216 159691 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
57400477 69741 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935588 69741 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
24763355 62626 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 4 4.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783604 62626 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 4 4.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
45487099 197691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1cccc(S(=O)(=O)c2cn(CCN)c3cccnc23)c1 10.1016/j.bmcl.2009.10.067
CHEMBL571215 197691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1cccc(S(=O)(=O)c2cn(CCN)c3cccnc23)c1 10.1016/j.bmcl.2009.10.067
56944186 112090 0 None -8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 8 1 7 4.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289984 112090 0 None -8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 8 1 7 4.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68108804 131689 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131689 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
90644513 111695 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286588 111695 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
11501251 94375 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 6 1 5 2.9 COC(=O)c1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL250804 94375 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 6 1 5 2.9 COC(=O)c1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
2303 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
4946 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
564 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
63 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
91536 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3187 68 None -346 26 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C nan
164628531 186464 0 None 5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4876727 186464 0 None 5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
44404394 132815 0 None -41 7 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL370128 132815 0 None -41 7 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
44386469 130678 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 428 6 0 6 3.9 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL368294 130678 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 428 6 0 6 3.9 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)cc1 10.1016/j.bmcl.2004.01.071
46214153 110695 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
CHEMBL3260334 110695 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
90644513 111695 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286588 111695 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
23655464 89387 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 330 5 1 5 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL236986 89387 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 330 5 1 5 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
90656168 110839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260801 110839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
66800934 112054 0 None -21 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 9 1 7 4.1 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289949 112054 0 None -21 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 9 1 7 4.1 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
68115856 132266 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 398 3 1 6 2.7 O=S(=O)(c1ccccc1)c1cc(N2CCOCC2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696979 132266 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 398 3 1 6 2.7 O=S(=O)(c1ccccc1)c1cc(N2CCOCC2)c2oc3c(c2c1)CNCC3 nan
127032424 139111 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786703 139111 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
168268877 189970 0 None -10 12 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189970 0 None -10 12 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
164624803 186212 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873127 186212 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164613297 184617 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4849230 184617 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
122377930 136652 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1016/j.ejmech.2015.11.040
CHEMBL3740054 136652 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1016/j.ejmech.2015.11.040
122377930 136652 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1039/C5MD00166H
CHEMBL3740054 136652 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1039/C5MD00166H
162651238 180266 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 238 2 0 4 1.5 CN(C)c1cccc2c1ccn2S(C)(=O)=O 10.1016/j.ejmech.2020.112916
CHEMBL4750554 180266 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 238 2 0 4 1.5 CN(C)c1cccc2c1ccn2S(C)(=O)=O 10.1016/j.ejmech.2020.112916
168275477 190451 0 None -263 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 388 9 5 7 3.1 Nc1nc(NCCNc2ccccc2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5178499 190451 0 None -263 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 388 9 5 7 3.1 Nc1nc(NCCNc2ccccc2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
145969402 164818 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4218625 164818 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
162644287 181790 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2020.112916
CHEMBL4777921 181790 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2020.112916
145975720 163960 0 None -229 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 394 4 1 4 2.5 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4207835 163960 0 None -229 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 394 4 1 4 2.5 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168268929 190030 0 None 3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 456 9 5 7 4.4 Nc1nc(NCCNc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5171734 190030 0 None 3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 456 9 5 7 4.4 Nc1nc(NCCNc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155515399 169957 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.9 CC(Cc1c[nH]c2ccccc12)NCc1ccc(-c2ccc(O)cc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4441691 169957 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.9 CC(Cc1c[nH]c2ccccc12)NCc1ccc(-c2ccc(O)cc2)o1 10.1016/j.ejmech.2019.111857
155557134 174537 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 493 10 0 5 5.1 CCOc1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4555890 174537 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 493 10 0 5 5.1 CCOc1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
118464425 138309 0 None -125 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 138309 0 None -125 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
58258834 128961 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 429 3 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669638 128961 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 429 3 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
44403088 140951 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL382297 140951 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
24763429 62627 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 4 1 5 4.1 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783605 62627 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 4 1 5 4.1 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
127047899 139811 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3cccc(C(F)(F)F)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798840 139811 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3cccc(C(F)(F)F)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
44242965 18761 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277916 18761 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
90656160 110831 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)n1 10.1016/j.bmcl.2014.03.049
CHEMBL3260792 110831 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)n1 10.1016/j.bmcl.2014.03.049
57395082 71544 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949766 71544 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963006 71544 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
56944191 112102 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 483 8 1 5 4.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289996 112102 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 483 8 1 5 4.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
25263334 179477 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 4.0 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1ccccc1 10.1016/j.bmcl.2009.03.077
CHEMBL474089 179477 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 4.0 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1ccccc1 10.1016/j.bmcl.2009.03.077
45378935 199505 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591939 199505 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
11729823 102971 1 None -95 5 Human 7.3 pKi = 7.3 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2cccc(I)c2)CC1 10.1021/jm0200411
CHEMBL306478 102971 1 None -95 5 Human 7.3 pKi = 7.3 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2cccc(I)c2)CC1 10.1021/jm0200411
134145903 148878 0 None -47 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3941529 148878 0 None -47 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
155541872 176685 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4519312 176685 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598357 176685 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
68281137 112080 0 None -22 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 9 1 7 3.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289974 112080 0 None -22 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 9 1 7 3.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
11630824 94340 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 4 1 6 2.0 CN1CCN(c2ccc([N+](=O)[O-])c(Nn3cccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250661 94340 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 4 1 6 2.0 CN1CCN(c2ccc([N+](=O)[O-])c(Nn3cccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
227584 158497 38 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4091082 158497 38 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
2771418 154165 33 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 1 6 1.8 Cc1cc(C)n(-c2cc(N3CCNCC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
CHEMBL398555 154165 33 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 1 6 1.8 Cc1cc(C)n(-c2cc(N3CCNCC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
164618100 185360 0 None 5 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 185360 0 None 5 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
71574300 86286 0 None -20 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312937 86286 0 None -20 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
162645383 179618 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4742713 179618 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
155562063 175751 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 8 2 3 5.5 CC(C)Oc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4583433 175751 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 8 2 3 5.5 CC(C)Oc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
156017281 177665 0 None -489 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 466 8 0 6 4.0 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4641609 177665 0 None -489 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 466 8 0 6 4.0 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
156018141 177921 0 None -1230 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 439 9 0 5 3.4 COc1ccccc1N1CCN(CCCCCCN2C(=O)[C@H]3[C@@H]4CC[C@@H](C4)[C@H]3C2=O)CC1 10.1016/j.bmc.2020.115459
CHEMBL4645292 177921 0 None -1230 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 439 9 0 5 3.4 COc1ccccc1N1CCN(CCCCCCN2C(=O)[C@H]3[C@@H]4CC[C@@H](C4)[C@H]3C2=O)CC1 10.1016/j.bmc.2020.115459
164620867 185642 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864448 185642 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
162666403 182392 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 306 3 0 4 3.2 CN(C)c1cccc2c1ccn2S(=O)(=O)C1CCCCC1 10.1016/j.ejmech.2020.112916
CHEMBL4785319 182392 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 306 3 0 4 3.2 CN(C)c1cccc2c1ccn2S(=O)(=O)C1CCCCC1 10.1016/j.ejmech.2020.112916
49783209 17609 0 None -245 26 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 0 None -245 26 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44581972 175600 0 None -16 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175600 0 None -16 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
138691366 174958 0 None -16 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2ccc(F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4565881 174958 0 None -16 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2ccc(F)cc12 10.1016/j.ejmech.2019.03.017
23857192 84392 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL2113365 84392 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL2219584 84392 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
44403056 70559 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1ccc(Cl)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194834 70559 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1ccc(Cl)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403066 168623 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 4 1 4 4.5 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL436124 168623 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 4 1 4 4.5 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10342674 6164 4 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)CC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081074 6164 4 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)CC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
145960391 161403 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4126633 161403 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
24777061 94862 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
CHEMBL253826 94862 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
137636699 156167 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 3 2 3 2.3 NC1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
CHEMBL4063897 156167 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 3 2 3 2.3 NC1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
45488166 196912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
CHEMBL566219 196912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
57391669 71562 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949677 71562 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963079 71562 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
56593803 65691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
CHEMBL1834346 65691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
11811724 116901 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 413 6 0 6 2.7 COc1ccc2c(c1)c(CCN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL338380 116901 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 413 6 0 6 2.7 COc1ccc2c(c1)c(CCN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
118731510 118247 0 None -16 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 9 1 4 5.4 NC(=O)c1ccccc1OCCCN1CCC(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409245 118247 0 None -16 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 9 1 4 5.4 NC(=O)c1ccccc1OCCCN1CCC(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
71463520 85300 2 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 2 2 1.6 CCc1[nH]c2ccncc2c1CCN 10.1007/s00044-004-0121-8
CHEMBL2260378 85300 2 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 2 2 1.6 CCc1[nH]c2ccncc2c1CCN 10.1007/s00044-004-0121-8
90656164 110835 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 2 1 4 1.8 O=C1CCCN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260797 110835 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 2 1 4 1.8 O=C1CCCN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
135367857 164604 0 None -30 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164604 0 None -30 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
57414790 131733 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 425 3 0 5 3.2 CS(=O)(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692952 131733 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 425 3 0 5 3.2 CS(=O)(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
168291393 191994 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 338 8 2 3 2.7 NC(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5201464 191994 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 338 8 2 3 2.7 NC(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
155520499 170484 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 494 9 0 6 4.6 O=[N+]([O-])c1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4449148 170484 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 494 9 0 6 4.6 O=[N+]([O-])c1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
145985585 165889 0 None -165 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249640 165889 0 None -165 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
162652195 180346 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 280 5 0 4 2.7 CCCCS(=O)(=O)n1ccc2c(N(C)C)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4751332 180346 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 280 5 0 4 2.7 CCCCS(=O)(=O)n1ccc2c(N(C)C)cccc21 10.1016/j.ejmech.2020.112916
44386911 131341 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 432 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Cl)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL368746 131341 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 432 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Cl)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
6918647 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
CHEMBL292759 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
58258756 127957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
6918647 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.01.031
CHEMBL292759 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.01.031
12017577 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2004.05.076
CHEMBL72554 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2004.05.076
9929294 64080 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180765 64080 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44388970 64856 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182099 64856 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
12017577 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/s0960-894x(00)00453-4
CHEMBL72554 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/s0960-894x(00)00453-4
44395595 67078 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
CHEMBL187278 67078 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
67156504 162150 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4161904 162150 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
145973178 163096 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4177024 163096 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
6918647 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm030030n
CHEMBL292759 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm030030n
12017577 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm030030n
CHEMBL72554 204500 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm030030n
2876391 208211 99 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 140 0 1 2 0.4 C1CCN2CCNCC2C1 10.1021/jm030030n
CHEMBL98511 208211 99 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 140 0 1 2 0.4 C1CCN2CCNCC2C1 10.1021/jm030030n
137636384 155951 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 356 4 0 4 2.5 CN(C)CC1=CC2=CN(S(=O)(=O)c3ccccc3)C3=CC=CC(O1)C23 10.1021/acsmedchemlett.6b00482
CHEMBL4061189 155951 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 356 4 0 4 2.5 CN(C)CC1=CC2=CN(S(=O)(=O)c3ccccc3)C3=CC=CC(O1)C23 10.1021/acsmedchemlett.6b00482
135398745 2914 112 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
47 2914 112 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
CHEMBL715 2914 112 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
DB00334 2914 112 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
155534670 171965 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4470718 171965 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
155513438 169729 0 None 4 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.8 Cc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4438434 169729 0 None 4 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.8 Cc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
164618879 185890 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4868468 185890 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
10319820 161195 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4073586 161195 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117715 161195 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
2435 3590 83 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
60149 3590 83 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
98 3590 83 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
CHEMBL12713 3590 83 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
DB06144 3590 83 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
44397689 71440 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196102 71440 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL373107 71440 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10272325 71741 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL196619 71741 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
44403099 133010 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370215 133010 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44435617 89142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236579 89142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9840311 5550 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076665 5550 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
46880658 6380 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1082199 6380 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
164613324 184677 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4849917 184677 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
127046819 139752 0 None 75 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 451 5 1 6 3.8 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc4[nH]ccc4c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798478 139752 0 None 75 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 451 5 1 6 3.8 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc4[nH]ccc4c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
57400234 71540 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71540 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71540 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
56944564 112059 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289954 112059 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
11396708 202211 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
CHEMBL609739 202211 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
11316594 202242 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
CHEMBL609993 202242 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
68108945 131632 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)c1cccc2ccccc12 nan
CHEMBL3692852 131632 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)c1cccc2ccccc12 nan
71462329 82035 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 406 3 0 4 4.1 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165539 82035 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 406 3 0 4 4.1 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
17940268 50285 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)c(Cl)cc2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157175 50285 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)c(Cl)cc2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328748 207693 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@H](C)N[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95511 207693 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@H](C)N[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918647 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 100746 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
44398251 68024 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1cccc2c(CCN)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm050247c
CHEMBL191385 68024 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1cccc2c(CCN)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm050247c
44435617 89142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236579 89142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162661903 181428 0 None -14 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
CHEMBL4764006 181428 0 None -14 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
46890293 7319 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 2 3 3.8 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ccc[nH]1 10.1016/j.bmcl.2010.03.110
CHEMBL1086114 7319 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 2 3 3.8 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ccc[nH]1 10.1016/j.bmcl.2010.03.110
46889327 7346 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 359 3 2 4 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc(F)cc4[nH]cnc34)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086251 7346 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 359 3 2 4 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc(F)cc4[nH]cnc34)ccc21 10.1016/j.bmcl.2010.03.110
17978376 69488 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 3 1 6 2.8 N#Cc1ccc2c(ccn2S(=O)(=O)c2cccc(Cl)c2)c1N1CCNCC1 10.1016/j.bmcl.2005.06.107
CHEMBL193379 69488 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 3 1 6 2.8 N#Cc1ccc2c(ccn2S(=O)(=O)c2cccc(Cl)c2)c1N1CCNCC1 10.1016/j.bmcl.2005.06.107
44441241 168924 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 1 4 3.8 CC1(C)CN(S(=O)(=O)c2cccc(F)c2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL438675 168924 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 1 4 3.8 CC1(C)CN(S(=O)(=O)c2cccc(F)c2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
10216820 85945 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL230069 85945 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2006.10.036
10173403 86430 0 None 3 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 426 4 1 3 4.8 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231430 86430 0 None 3 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 426 4 1 3 4.8 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
44425699 150568 7 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 1 3 3.8 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CN(C)C3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL395501 150568 7 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 1 3 3.8 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CN(C)C3)cc1 10.1016/j.bmcl.2006.10.036
9892409 100950 0 None 63 9 Human 8.3 pKi = 8.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 100950 0 None 63 9 Human 8.3 pKi = 8.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
71451603 82044 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165547 82044 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
135398737 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 93 None -4 89 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44386821 61568 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc3ccccc3c2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL177107 61568 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc3ccccc3c2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
58258833 127968 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127968 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
66801160 112052 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289947 112052 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68109436 131645 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccccc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692865 131645 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccccc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
68115681 131728 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692947 131728 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
56593932 65693 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
CHEMBL1834348 65693 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
10068007 18787 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278090 18787 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
44474625 14071 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197521 14071 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL575270 14071 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
10113751 62113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL177605 62113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm5003952
10202396 60481 3 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL175471 60481 3 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
10113751 62113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL177605 62113 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
44544599 178216 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 3 1 6 2.4 CC(=O)N1CCc2ccc(NS(=O)(=O)c3c(Cl)nc4n3CCS4)cc21 10.1016/j.ejmech.2018.11.017
CHEMBL4649783 178216 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 3 1 6 2.4 CC(=O)N1CCc2ccc(NS(=O)(=O)c3c(Cl)nc4n3CCS4)cc21 10.1016/j.ejmech.2018.11.017
71502632 118264 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 493 8 0 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409262 118264 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 493 8 0 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
68115685 131712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1CO nan
CHEMBL3692931 131712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1CO nan
16049388 82023 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165527 82023 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435609 154402 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL398808 154402 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
20901117 10676 3 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10676 3 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44435609 154402 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398808 154402 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16222652 82039 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 500 3 0 4 5.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165542 82039 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 500 3 0 4 5.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
10380133 198336 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL576315 198336 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836508 18770 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
CHEMBL1277998 18770 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
1588 2325 27 None -21 44 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 27 None -21 44 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 27 None -21 44 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 27 None -21 44 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 27 None -21 44 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
25024524 62934 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1784917 62934 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
129103318 167314 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
CHEMBL4293999 167314 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
129103318 167314 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167314 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
25024928 62967 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 5 3.2 O=S(=O)(c1ccc(F)cc1F)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785071 62967 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 5 3.2 O=S(=O)(c1ccc(F)cc1F)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
58258785 127926 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5c(F)cccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664750 127926 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5c(F)cccc54)ccc31)C1CCC(C2)N1 nan
129103161 167070 0 None -51 13 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.bmcl.2021.127909
CHEMBL4289498 167070 0 None -51 13 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.bmcl.2021.127909
56593646 65683 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834338 65683 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
44435615 89141 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236578 89141 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57398718 69745 0 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69745 0 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
46880607 5974 1 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079977 5974 1 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
68115642 131727 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692946 131727 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
68115771 131743 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1ccc(C2CCOC2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692962 131743 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1ccc(C2CCOC2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
44435615 89141 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236578 89141 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
11350253 114167 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 405 3 1 6 3.0 O=c1n(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm5003952
CHEMBL3329437 114167 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 405 3 1 6 3.0 O=c1n(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm5003952
44395451 66263 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184652 66263 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
45113530 14223 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095274 14223 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199079 14223 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
137648172 157810 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4083289 157810 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137628796 160989 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4105377 160989 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116137 160989 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44435626 154858 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
CHEMBL400608 154858 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
9865474 175119 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45695 175119 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
68115878 132259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 3 2 5 3.0 CC(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696972 132259 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 3 2 5 3.0 CC(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
54580442 62935 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.0 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
CHEMBL1784918 62935 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.0 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
44435626 154858 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.ejmech.2010.05.045
CHEMBL400608 154858 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.ejmech.2010.05.045
162657983 181048 0 None -23 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
CHEMBL4759492 181048 0 None -23 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
52913220 127909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 4 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664733 127909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 4 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)F)c4)ccc31)C1CCC(C2)N1 nan
68341955 127949 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5cc[nH]c5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664774 127949 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5cc[nH]c5c4)ccc31)C1CCC(C2)N1 nan
58258833 127968 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127968 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
58158739 139157 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787201 139157 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
25263347 184126 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccccc2Cl)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482737 184126 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccccc2Cl)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25025314 62932 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 6 0 5 4.1 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C(C)C)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1784915 62932 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 6 0 5 4.1 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C(C)C)cc3)c2)CC1 10.1021/ml100101u
16222866 82054 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 398 4 0 5 3.6 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165557 82054 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 398 4 0 5 3.6 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
68115651 131708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692927 131708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
44388980 64495 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 459 6 2 6 4.4 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181425 64495 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 459 6 2 6 4.4 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44401465 69852 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 293 5 1 3 3.4 CN(C)CCn1cc(Cc2ccc(N)cc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL193841 69852 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 293 5 1 3 3.4 CN(C)CCn1cc(Cc2ccc(N)cc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
5 139 72 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 72 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 72 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 72 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
11849199 77882 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL209383 77882 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
6918531 112233 12 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 365 3 3 3 3.3 Nc1ccc(S(=O)(=O)Nc2cc(Br)cc3[nH]ccc23)cc1 10.1021/jm030030n
CHEMBL329075 112233 12 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 365 3 3 3 3.3 Nc1ccc(S(=O)(=O)Nc2cc(Br)cc3[nH]ccc23)cc1 10.1021/jm030030n
44568063 183013 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 0 5 3.3 CCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL479374 183013 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 0 5 3.3 CCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
162645783 179600 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 11 1 7 5.1 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4742220 179600 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 11 1 7 5.1 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
137629291 161008 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4079871 161008 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116243 161008 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
54583109 62533 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782358 62533 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
11849199 77882 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL209383 77882 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
155522487 170677 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 428 5 2 6 3.4 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4451666 170677 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 428 5 2 6 3.4 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155556757 176264 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
CHEMBL4557068 176264 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
CHEMBL4594991 176264 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
24763354 62624 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 369 3 1 4 3.5 Cc1cccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)c1 10.1016/j.bmcl.2009.04.108
CHEMBL1783602 62624 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 369 3 1 4 3.5 Cc1cccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)c1 10.1016/j.bmcl.2009.04.108
25263298 184125 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2c(cnn2S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.bmcl.2009.03.071
CHEMBL482736 184125 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2c(cnn2S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.bmcl.2009.03.071
25263330 181007 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1ccc(Cl)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL475902 181007 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1ccc(Cl)cc1 10.1016/j.bmcl.2009.03.077
68115775 132246 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 374 2 1 5 3.1 N#Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696959 132246 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 374 2 1 5 3.1 N#Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
11307899 78868 0 None -794 7 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
CHEMBL2112882 78868 0 None -794 7 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
6918515 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
71 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
CHEMBL7318 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
11190151 130178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
CHEMBL367832 130178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
11014674 161940 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm050247c
CHEMBL415464 161940 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm050247c
44328120 208036 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm050247c
CHEMBL97492 208036 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm050247c
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
134129927 142414 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2c3c(ccc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
CHEMBL3889852 142414 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2c3c(ccc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
2726 919 68 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 919 68 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 919 68 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 919 68 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 919 68 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
44425698 86293 7 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 330 6 2 3 3.4 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL231326 86293 7 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 330 6 2 3 3.4 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNC3)cc1 10.1016/j.bmcl.2006.10.036
44425711 86528 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 504 4 1 3 5.6 CN1CCc2cc(Br)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231546 86528 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 504 4 1 3 5.6 CN1CCc2cc(Br)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
44425714 86678 0 None -19 5 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 460 4 1 3 5.5 CN1CCc2cc(Cl)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231648 86678 0 None -19 5 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 460 4 1 3 5.5 CN1CCc2cc(Cl)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
156009804 177052 0 None - 1 Human 6.3 pKi = 6.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 424 4 2 6 3.7 O=S(=O)(Nc1ccc2sc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.ejmech.2018.11.017
CHEMBL4632617 177052 0 None - 1 Human 6.3 pKi = 6.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 424 4 2 6 3.7 O=S(=O)(Nc1ccc2sc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.ejmech.2018.11.017
155541676 173059 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4519436 173059 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
44568102 184023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 460 6 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(CCc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482099 184023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 460 6 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(CCc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
71458651 81434 0 None -50 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159477 81434 0 None -50 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
57399868 71556 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949978 71556 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963032 71556 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
164610456 184500 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4847379 184500 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
156014787 177545 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640281 177545 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
4189 206922 96 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 96 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 96 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
168282454 191215 0 None -63 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 485 11 4 8 3.6 Nc1nc(NCCCCN2CCN(c3ccccc3)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5189648 191215 0 None -63 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 485 11 4 8 3.6 Nc1nc(NCCCCN2CCN(c3ccccc3)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
3198 205513 76 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 76 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 76 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
155531846 171645 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 300 4 1 7 0.8 CN1CCN(c2nc(N)nc(COc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4465929 171645 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 300 4 1 7 0.8 CN1CCN(c2nc(N)nc(COc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
155524957 176345 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4455845 176345 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595569 176345 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
68115847 132256 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 5 2 6 3.1 CC(C)(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696969 132256 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 5 2 6 3.1 CC(C)(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44403095 135234 0 None -2818 6 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL372453 135234 0 None -2818 6 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
57392614 70768 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950770 70768 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 nan
162663184 181996 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 596 12 1 7 5.5 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4780498 181996 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 596 12 1 7 5.5 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
164616670 184613 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4849077 184613 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
57392614 70768 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950770 70768 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
16718827 175409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
CHEMBL457570 175409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
11384675 63193 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049615n
CHEMBL179034 63193 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049615n
44263956 204448 1 None 2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm990550b
CHEMBL7220 204448 1 None 2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm990550b
118736375 118947 0 None -19 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 477 6 0 9 2.2 Cc1cccc(N2CCN(CCCCn3c(C)cn4c5c(=O)n(C)c(=O)n(C)c5nc34)CC2)c1C 10.1016/j.ejmech.2015.04.046
CHEMBL3423339 118947 0 None -19 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 477 6 0 9 2.2 Cc1cccc(N2CCN(CCCCn3c(C)cn4c5c(=O)n(C)c(=O)n(C)c5nc34)CC2)c1C 10.1016/j.ejmech.2015.04.046
56593799 65689 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834343 65689 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
17055181 162452 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 409 7 1 2 6.2 Cc1ccc(COc2ccc(Br)cc2CNC(C)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4166667 162452 1 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 409 7 1 2 6.2 Cc1ccc(COc2ccc(Br)cc2CNC(C)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.010
275 3360 9 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
3246 3360 9 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
5312144 3360 9 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
CHEMBL46071 3360 9 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
71453280 81440 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159483 81440 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
13069602 120612 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360996 120612 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546112 120612 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57399548 70753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950754 70753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
58258869 128995 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(N4CCCC4)c31)C1CCC(C2)N1 nan
CHEMBL3669672 128995 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(N4CCCC4)c31)C1CCC(C2)N1 nan
12 1553 17 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1553 17 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1553 17 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
11849745 79843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212178 79843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
6761 67799 19 None -9 18 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 19 None -9 18 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
137654850 158971 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 341 3 1 5 3.0 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00482
CHEMBL4096141 158971 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 341 3 1 5 3.0 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00482
137650191 157191 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4075727 157191 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
156014079 177256 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2ccccc12 10.1016/j.bmc.2020.115459
CHEMBL4636031 177256 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2ccccc12 10.1016/j.bmc.2020.115459
57399548 70753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950754 70753 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11849745 79843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
CHEMBL212178 79843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
24783295 176790 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2oc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
CHEMBL460626 176790 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2oc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
118731503 118235 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 555 9 1 6 5.7 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409233 118235 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 555 9 1 6 5.7 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118731507 118238 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 11 2 6 4.8 O=C1CCc2ccc(OCCCCNCCc3cn(S(=O)(=O)c4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409236 118238 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 11 2 6 4.8 O=C1CCc2ccc(OCCCCNCCc3cn(S(=O)(=O)c4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
57391618 71469 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71469 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71469 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
11190151 130178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367832 130178 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
56944086 112082 0 None -999 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 420 8 1 7 2.8 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289976 112082 0 None -999 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 420 8 1 7 2.8 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
4601 206747 35 None -2 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 206747 35 None -2 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 206747 35 None -2 16 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
155525596 171059 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 2 4 4.9 Oc1ccc(-c2ccc(CNCCc3coc4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4457045 171059 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 2 4 4.9 Oc1ccc(-c2ccc(CNCCc3coc4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
68109040 131678 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 2.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNC(CO)C3 nan
CHEMBL3692897 131678 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 2.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNC(CO)C3 nan
49781471 17761 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 533 8 2 8 4.3 COc1ccc(NS(=O)(=O)c2ccc(-c3ncc(-c4ccc(N(C)C)cc4)o3)cc2)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1258714 17761 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 533 8 2 8 4.3 COc1ccc(NS(=O)(=O)c2ccc(-c3ncc(-c4ccc(N(C)C)cc4)o3)cc2)cc1N1CCNCC1 10.1021/jm1007177
8431 1484 9 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
9843179 1484 9 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
CHEMBL69257 1484 9 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
162657889 181057 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCN(CC(F)(F)F)CC3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4759633 181057 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCN(CC(F)(F)F)CC3)ccc21 10.1016/j.ejmech.2020.112916
155534301 171935 0 None -123 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 415 8 0 5 4.0 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4470304 171935 0 None -123 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 415 8 0 5 4.0 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2019.06.029
156009734 177166 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 393 5 2 4 3.7 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4634426 177166 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 393 5 2 4 3.7 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
155555200 174363 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.2 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4551512 174363 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.2 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
145975992 163516 0 None -20 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 393 4 1 3 3.6 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4202520 163516 0 None -20 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 393 4 1 3 3.6 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
142601329 186517 5 None -79 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 186517 5 None -79 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
16118924 60151 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642855 60151 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739686 60151 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
164619932 186207 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 386 8 1 3 4.3 Cc1cccc(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4873096 186207 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 386 8 1 3 4.3 Cc1cccc(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
16718917 181682 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 181682 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
66801140 111662 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3286432 111662 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68108927 131648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692868 131648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
24966736 84026 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207377 84026 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
11014674 161940 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm021085c
CHEMBL415464 161940 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm021085c
4407909 192866 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192866 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192866 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
1530 2182 50 None -58 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2182 50 None -58 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2182 50 None -58 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2182 50 None -58 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2182 50 None -58 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
155557890 174705 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 333 6 3 4 3.9 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4559790 174705 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 333 6 3 4 3.9 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncccc34)o2)cc1 10.1016/j.ejmech.2019.111857
68109274 131659 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692878 131659 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
156013203 177482 0 None -16 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
CHEMBL4639203 177482 0 None -16 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
71449645 81447 0 None -21 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159490 81447 0 None -21 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
127025242 137802 0 None -269 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2cccc(F)c2)C3)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759617 137802 0 None -269 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2cccc(F)c2)C3)c1 10.1016/j.ejmech.2015.11.040
44390095 11745 21 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1181566 11745 21 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL180298 11745 21 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44388986 64774 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 438 3 0 5 4.9 CC(C)(C)OC(=O)N1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL181938 64774 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 438 3 0 5 4.9 CC(C)(C)OC(=O)N1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
9796627 96653 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 96653 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
6918515 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2612 38 None 4 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
162660390 181230 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 570 12 0 7 4.9 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4761469 181230 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 570 12 0 7 4.9 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
57397900 70752 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 338 2 2 3 3.4 O=S(=O)(c1ccccc1)c1ccc2[nH]c3c(c2c1)C1CCC(C3)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950753 70752 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 338 2 2 3 3.4 O=S(=O)(c1ccccc1)c1ccc2[nH]c3c(c2c1)C1CCC(C3)N1 10.1016/j.bmcl.2012.01.022
127045873 140024 0 None 22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 438 3 0 6 3.3 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(C)(=O)=O)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3800153 140024 0 None 22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 438 3 0 6 3.3 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(C)(=O)=O)c3n2)CC1 10.1016/j.bmcl.2016.04.024
24784069 191105 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1cccc(F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518781 191105 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1cccc(F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
90656153 110824 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260785 110824 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
66800916 112067 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 518 8 1 7 4.8 Cc1c(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289962 112067 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 518 8 1 7 4.8 Cc1c(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
45378934 201646 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 201646 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
11638332 94924 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 319 1 1 2 4.1 CC1(c2ccccc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL254298 94924 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 319 1 1 2 4.1 CC1(c2ccccc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
CHEMBL5076882 214466 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cccc(Cl)c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
44328120 208036 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm030030n
CHEMBL97492 208036 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm030030n
135 2532 43 None -21 58 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
1796 2532 43 None -21 58 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
4184 2532 43 None -21 58 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
CHEMBL6437 2532 43 None -21 58 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
DB06148 2532 43 None -21 58 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
155511262 169544 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cccc(O)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4435528 169544 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cccc(O)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
164625686 186319 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 3.9 O=C1Cc2c(OCCNCc3ccccc3)cccc2N1Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4874675 186319 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 3.9 O=C1Cc2c(OCCNCc3ccccc3)cccc2N1Cc1ccccc1 10.1016/j.ejmech.2021.113792
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
24763350 62621 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 355 3 1 4 3.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccccc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783599 62621 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 355 3 1 4 3.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccccc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
274 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
5312145 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
CHEMBL433461 3339 44 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
90656163 110834 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(N3CCNCC3)ccnc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260796 110834 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(N3CCNCC3)ccnc2c1 10.1016/j.bmcl.2014.03.049
57396813 71545 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71545 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71545 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68115734 132258 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 3 2 5 3.1 CC(C)(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696971 132258 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 3 2 5 3.1 CC(C)(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
11475760 120498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm049615n
CHEMBL354418 120498 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm049615n
23652922 56697 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 431 4 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642428 56697 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 431 4 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2010.11.001
137653132 158906 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 401 4 0 5 3.1 Cc1c(CN2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4095446 158906 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 401 4 0 5 3.1 Cc1c(CN2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
44397117 13023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1189862 13023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL539587 13023 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
155512944 169719 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 249 1 1 2 3.4 Cn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4438349 169719 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 249 1 1 2 3.4 Cn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
71453282 81448 0 None -69 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159491 81448 0 None -69 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
49781254 17186 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 772 16 2 9 6.6 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256258 17186 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 772 16 2 9 6.6 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
71574298 86285 0 None -13 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 526 8 1 5 5.1 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312936 86285 0 None -13 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 526 8 1 5 5.1 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
145976408 163878 0 None -83 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 424 5 1 4 3.4 O=C1Nc2ccccc2C12CCN(CCCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4206881 163878 0 None -83 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 424 5 1 4 3.4 O=C1Nc2ccccc2C12CCN(CCCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
155532887 171808 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 7 1 4 4.8 COc1cccc(-c2ccc(CNCCc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4468235 171808 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 7 1 4 4.8 COc1cccc(-c2ccc(CNCCc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155543192 173287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4525628 173287 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
134949378 181490 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccccc3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4764769 181490 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccccc3)ccc21 10.1016/j.ejmech.2020.112916
127025243 137743 0 None -562 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759205 137743 0 None -562 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
137649536 157301 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4077077 157301 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2017.04.033
126720443 162964 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 5 1 5 2.8 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4174854 162964 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 5 1 5 2.8 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
45487113 197752 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 371 6 0 6 2.6 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccccc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571635 197752 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 371 6 0 6 2.6 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccccc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
57391569 71525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949929 71525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962864 71525 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
66801335 112053 0 None -5 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 8 1 7 3.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289948 112053 0 None -5 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 8 1 7 3.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
68108832 131675 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131675 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
90644078 112089 0 None -18 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 490 7 1 7 4.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289983 112089 0 None -18 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 490 7 1 7 4.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
2880253 162707 9 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
CHEMBL4170813 162707 9 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
134155476 151225 0 None -53 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3960056 151225 0 None -53 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
57391620 71565 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949769 71565 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963098 71565 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
5640104 117939 11 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 429 4 1 5 3.4 NC(=O)C1CCN(c2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2015.03.049
CHEMBL3403342 117939 11 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 429 4 1 5 3.4 NC(=O)C1CCN(c2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2015.03.049
156012551 177337 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 8 0 5 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4637294 177337 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 8 0 5 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
44390011 12252 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1184633 12252 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL360663 12252 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44401434 166349 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 275 4 0 1 4.6 CN(C)CCC1=C/C(=C\c2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL427354 166349 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 275 4 0 1 4.6 CN(C)CCC1=C/C(=C\c2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
44395604 66725 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)c2cn(CCN(C)C)c3ccccc23)cc1 10.1016/j.bmcl.2004.09.003
CHEMBL185672 66725 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)c2cn(CCN(C)C)c3ccccc23)cc1 10.1016/j.bmcl.2004.09.003
16118925 60152 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642856 60152 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739694 60152 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
156019543 177936 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2020.115459
CHEMBL4645525 177936 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2020.115459
126720426 162807 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cc(F)ccc1F 10.1016/j.ejmech.2017.12.053
CHEMBL4172424 162807 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cc(F)ccc1F 10.1016/j.ejmech.2017.12.053
118731511 118248 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 9 1 6 4.6 NC(=O)c1ccccc1OCCCN1CCC(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409246 118248 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 9 1 6 4.6 NC(=O)c1ccccc1OCCCN1CCC(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
11750876 201797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
CHEMBL606870 201797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
11234781 120421 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL353739 120421 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
44387804 131382 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 5.5 Cc1c(S(=O)(=O)Nc2cccc3c2cc(C)n3CCN(C)C)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL368973 131382 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 5.5 Cc1c(S(=O)(=O)Nc2cccc3c2cc(C)n3CCN(C)C)sc2ccc(Cl)cc12 10.1021/jm049615n
2816054 110823 22 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 1 1 3 2.6 O=C1CSC2(C(=O)Nc3ccccc32)N1c1ccccc1 10.1016/j.bmcl.2014.03.049
CHEMBL3260784 110823 22 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 1 1 3 2.6 O=C1CSC2(C(=O)Nc3ccccc32)N1c1ccccc1 10.1016/j.bmcl.2014.03.049
155534575 171946 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 429 8 0 7 2.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4470487 171946 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 429 8 0 7 2.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
68109126 131662 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCCC3 nan
CHEMBL3692881 131662 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCCC3 nan
242 470 124 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
34 470 124 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
60795 470 124 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
CHEMBL1112 470 124 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
DB01238 470 124 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
168277374 190369 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 441 8 4 6 4.6 Nc1nc(NCCc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5177186 190369 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 441 8 4 6 4.6 Nc1nc(NCCc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
6090 34567 19 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.08.068
CHEMBL142936 34567 19 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.08.068
164615340 185429 0 None 3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4861431 185429 0 None 3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155518974 170350 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)cc1 10.1016/j.bmcl.2019.06.029
CHEMBL4447330 170350 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)cc1 10.1016/j.bmcl.2019.06.029
274 3339 44 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
5312145 3339 44 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
CHEMBL433461 3339 44 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
155556168 174427 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 365 5 1 7 2.0 COc1ccc(Cc2nc(N3CCNCC3)nc3cccnc23)c(OC)c1 10.1016/j.ejmech.2019.111857
CHEMBL4552950 174427 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 365 5 1 7 2.0 COc1ccc(Cc2nc(N3CCNCC3)nc3cccnc23)c(OC)c1 10.1016/j.ejmech.2019.111857
137645440 157998 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4085349 157998 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44403091 140357 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 357 3 1 6 2.9 Cc1nc(C)c(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)o1 10.1016/j.bmcl.2005.07.028
CHEMBL380777 140357 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 357 3 1 6 2.9 Cc1nc(C)c(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)o1 10.1016/j.bmcl.2005.07.028
45488131 198581 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
CHEMBL578411 198581 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
9945214 82017 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counterDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counter
ChEMBL 326 2 2 3 2.8 NC1CCc2[nH]c3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165521 82017 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counterDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counter
ChEMBL 326 2 2 3 2.8 NC1CCc2[nH]c3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 10.1016/j.bmcl.2012.06.002
11589069 96247 0 None -354 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 96247 0 None -354 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
2867758 162042 7 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 339 6 1 2 5.5 Cc1ccc(C(C)(C)CC(C)NCc2ccc(C(F)(F)F)cc2)o1 10.1016/j.ejmech.2018.04.010
CHEMBL4160177 162042 7 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 339 6 1 2 5.5 Cc1ccc(C(C)(C)CC(C)NCc2ccc(C(F)(F)F)cc2)o1 10.1016/j.ejmech.2018.04.010
118729733 117934 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 394 4 1 3 5.4 O=S(=O)(Nc1ccccc1-c1nccc2ccccc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403338 117934 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 394 4 1 3 5.4 O=S(=O)(Nc1ccccc1-c1nccc2ccccc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2015.03.049
58258846 128992 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 453 5 1 6 2.8 CN(C)C(=O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669669 128992 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 453 5 1 6 2.8 CN(C)C(=O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
168277502 190715 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 468 8 0 5 6.2 S=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5182383 190715 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 468 8 0 5 6.2 S=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
2812 4779 101 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 101 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
23906630 117929 5 None 2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 1 2 2.9 O=S(=O)(c1ccc(F)cc1)N1CC=c2ccccc2=C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403333 117929 5 None 2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 1 2 2.9 O=S(=O)(c1ccc(F)cc1)N1CC=c2ccccc2=C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
168273001 190212 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 403 9 4 7 3.3 COc1ccccc1CCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5174637 190212 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 403 9 4 7 3.3 COc1ccccc1CCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155549153 174234 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 420 3 0 6 3.4 CC(=O)N1CCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4548837 174234 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 420 3 0 6 3.4 CC(=O)N1CCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
155563286 175327 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cc(F)ccc12 10.1016/j.ejmech.2019.03.017
CHEMBL4573883 175327 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cc(F)ccc12 10.1016/j.ejmech.2019.03.017
11695841 114174 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 5 2 3 3.7 N=C(N)CCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1021/jm5003952
CHEMBL3329444 114174 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 5 2 3 3.7 N=C(N)CCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1021/jm5003952
4494260 154649 15 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 360 5 1 5 3.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(Cl)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL399478 154649 15 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 360 5 1 5 3.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(Cl)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
137656602 159601 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103190 159601 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
44438689 148818 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 5 0 4 2.3 CC(C)S(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL394097 148818 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 5 0 4 2.3 CC(C)S(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
57395598 68425 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917346 68425 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
156018601 177894 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 414 6 1 5 3.4 C=CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4644833 177894 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 414 6 1 5 3.4 C=CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
118731508 118245 0 None -19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 465 9 1 4 5.3 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409243 118245 0 None -19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 465 9 1 4 5.3 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
118464427 138334 0 None -213 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 138334 0 None -213 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
71727069 102405 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL2401935 102405 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3039672 102405 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
155560272 175086 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 476 4 1 5 3.6 CC1=CC=CN2C(=O)C3C=C(S(=O)(=O)c4ccccc4)C(=N)N(Cc4ccc(F)cc4)C3N=C12 10.1016/j.ejmech.2019.111857
CHEMBL4568668 175086 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 476 4 1 5 3.6 CC1=CC=CN2C(=O)C3C=C(S(=O)(=O)c4ccccc4)C(=N)N(Cc4ccc(F)cc4)C3N=C12 10.1016/j.ejmech.2019.111857
118731351 118188 0 None -30 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409035 118188 0 None -30 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
122483292 138111 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 138111 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 138111 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
155533704 171859 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 383 2 2 2 3.8 CN1C=C2C(NC(=S)NC2c2ccc(F)cc2)/C(=C\c2ccc(F)cc2)C1 10.1016/j.ejmech.2019.111857
CHEMBL4469065 171859 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 383 2 2 2 3.8 CN1C=C2C(NC(=S)NC2c2ccc(F)cc2)/C(=C\c2ccc(F)cc2)C1 10.1016/j.ejmech.2019.111857
2737389 187586 28 None -426 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 187586 28 None -426 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
71574304 86265 0 None -22 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2cccnc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312638 86265 0 None -22 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2cccnc12 10.1016/j.ejmech.2012.11.042
448537 160250 89 None -35 25 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 160250 89 None -35 25 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44397102 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.05.076
CHEMBL188144 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.05.076
23757269 114453 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.bmcl.2004.05.076
CHEMBL333373 114453 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.bmcl.2004.05.076
44397102 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL188144 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
44397102 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
CHEMBL188144 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
126720440 163026 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4175829 163026 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
44397102 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL188144 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
155525318 170988 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
CHEMBL4456224 170988 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
164618100 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4860275 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
164620748 186245 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4873623 186245 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
67156504 162150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.1c00224
CHEMBL4161904 162150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.1c00224
126720440 163026 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175829 163026 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
134130413 142234 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 579 8 1 7 5.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884618 142234 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 579 8 1 7 5.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
9979009 159095 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4097459 159095 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
10317027 161062 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4062687 161062 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116630 161062 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
164618100 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164620748 186245 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873623 186245 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
46880757 6028 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080381 6028 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
46880486 6170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081095 6170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164612180 184741 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4850764 184741 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164611496 185457 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 563 8 1 7 5.6 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)C1 10.1016/j.ejmech.2021.113792
CHEMBL4861756 185457 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 563 8 1 7 5.6 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)C1 10.1016/j.ejmech.2021.113792
164623148 185549 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 424 8 1 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863101 185549 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 424 8 1 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113792
44397102 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1021/jm8009469
CHEMBL188144 67269 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1021/jm8009469
23655289 88689 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL235986 88689 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
23655468 89391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236989 89391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
127045874 139845 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 4 0 6 4.1 CC(C)S(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799120 139845 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 4 0 6 4.1 CC(C)S(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
23655468 89391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/acs.jmedchem.5b00179
CHEMBL236989 89391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/acs.jmedchem.5b00179
57414664 131720 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.9 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692939 131720 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.9 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
164618100 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 185360 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
135398737 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
38 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
722 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
CHEMBL42 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
DB00363 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
58158749 138995 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785512 138995 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
135398737 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
38 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
722 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
CHEMBL42 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
DB00363 958 93 None -4 89 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
44435646 145560 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL391517 145560 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
68115646 131742 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1C(F)(F)F nan
CHEMBL3692961 131742 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1C(F)(F)F nan
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
44435646 145560 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL391517 145560 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
23757269 114453 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL333373 114453 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
66801158 112084 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289978 112084 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
57414394 131623 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692843 131623 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
52913228 70763 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950764 70763 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 nan
16117278 60149 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642884 60149 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739659 60149 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
52913228 70763 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950764 70763 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
1621 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
17 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
5761 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
CHEMBL263881 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
DB04829 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
9849116 207583 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2c(Cl)cc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL94930 207583 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2c(Cl)cc(Cl)cc12 10.1016/s0960-894x(01)00558-3
44398577 133464 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 301 3 2 5 1.9 NCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
CHEMBL370672 133464 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 301 3 2 5 1.9 NCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
46890323 6907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 402 4 1 4 2.5 O=C1CN(C[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)CCN1 10.1016/j.bmcl.2010.03.110
CHEMBL1084335 6907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 402 4 1 4 2.5 O=C1CN(C[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)CCN1 10.1016/j.bmcl.2010.03.110
10295001 135217 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL372287 135217 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
44425704 85946 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 412 4 1 4 4.6 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccc4c(c3)CCN(C)CC4)cc2)s1 10.1016/j.bmcl.2006.10.036
CHEMBL230070 85946 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 412 4 1 4 4.6 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccc4c(c3)CCN(C)CC4)cc2)s1 10.1016/j.bmcl.2006.10.036
129103322 167373 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4294799 167373 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
66803474 156316 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4065568 156316 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
118654428 191757 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5197660 191757 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
56593931 65692 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
CHEMBL1834347 65692 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
25263338 184168 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 344 5 1 3 5.0 CCC(Oc1nccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL482988 184168 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 344 5 1 3 5.0 CCC(Oc1nccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
67085495 127913 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 3.4 CNc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664737 127913 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 3.4 CNc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
3028929 208160 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 6 0 3 3.8 COc1ccc2c(c1)c(CCN(C)C)cn2Cc1ccccc1 10.1021/jm030030n
CHEMBL98237 208160 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 6 0 3 3.8 COc1ccc2c(c1)c(CCN(C)C)cn2Cc1ccccc1 10.1021/jm030030n
53327611 69754 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69754 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
164624187 185846 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4867606 185846 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
25263343 184150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(COc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482938 184150 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(COc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
56944383 112119 0 None -9 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 112119 0 None -9 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
57414388 131620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692840 131620 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
16071727 60102 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642848 60102 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739253 60102 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
16117154 60147 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642881 60147 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739657 60147 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
137651613 157172 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 6 0 6 3.8 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4075502 157172 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 6 0 6 3.8 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
10275386 63912 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 445 5 2 3 5.4 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(-c5ccccc5)cc4)cc23)CC1 10.1021/jm049615n
CHEMBL180582 63912 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 445 5 2 3 5.4 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(-c5ccccc5)cc4)cc23)CC1 10.1021/jm049615n
16223064 82059 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 430 5 0 6 4.0 COc1ccc(S(=O)(=O)n2c3c(c4cc(SC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165562 82059 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 430 5 0 6 4.0 COc1ccc(S(=O)(=O)n2c3c(c4cc(SC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
67085507 127936 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 450 3 1 5 4.6 Cc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664760 127936 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 450 3 1 5 4.6 Cc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
1621 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2429 17 None -16 45 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5113605 79723 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1021/jm060469q
CHEMBL211577 79723 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1021/jm060469q
44327999 112402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
44327999 112402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL329739 112402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL329739 112402 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
21071390 1987 53 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
8689 1987 53 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
CHEMBL3286580 1987 53 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
DB11957 1987 53 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
137630883 161124 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4073450 161124 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117188 161124 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
57396970 69743 0 None -4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69743 0 None -4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
71151929 118265 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 0 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409263 118265 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 0 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
25263320 188845 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL506736 188845 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
52912975 70757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950758 70757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 nan
15480742 13024 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL1189863 13024 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL539589 13024 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
49756 204312 13 None 2 8 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL7143 204312 13 None 2 8 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030030n
44476704 82343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172182 82343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
49756 204312 13 None 2 8 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 204312 13 None 2 8 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
137635884 155900 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 427 7 2 3 4.1 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4060649 155900 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 427 7 2 3 4.1 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
118626140 165918 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250244 165918 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
155515318 169984 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 3 3 5.1 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(Cl)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4442111 169984 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 3 3 5.1 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(Cl)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
2726 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
52912975 70757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950758 70757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
10274390 184798 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 431 5 0 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(Cc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4851655 184798 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 431 5 0 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(Cc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2021.113792
155555224 174349 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4551220 174349 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
68115743 132265 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1ccc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)n1 nan
CHEMBL3696978 132265 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1ccc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)n1 nan
2726 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 919 68 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
44476704 82343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172182 82343 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
44386815 61772 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 2 1 4 3.8 COc1ccc2c(c1)c1c(n2C(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
CHEMBL177233 61772 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 2 1 4 3.8 COc1ccc2c(c1)c1c(n2C(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
44386665 131347 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 306 3 1 3 4.2 COc1ccc2c(c1)c1c(n2Cc2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
CHEMBL368783 131347 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 306 3 1 3 4.2 COc1ccc2c(c1)c1c(n2Cc2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
1353 1911 93 None -1047 83 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 1911 93 None -1047 83 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 1911 93 None -1047 83 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 1911 93 None -1047 83 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 1911 93 None -1047 83 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
44438743 151383 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 2 1 2 4.2 Nc1ccc(Cn2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL396149 151383 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 2 1 2 4.2 Nc1ccc(Cn2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL4748908 214035 1 None -6 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of 5-HT6GPCRScan assay: inhibition of 5-HT6
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
155540147 172928 0 None 14 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 233 1 1 2 2.8 Cn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4516621 172928 0 None 14 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 233 1 1 2 2.8 Cn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
118731354 118190 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 10 0 4 4.9 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(=O)N2CCCCC2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409037 118190 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 10 0 4 4.9 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(=O)N2CCCCC2)CC1 10.1016/j.ejmech.2014.12.041
2600 3779 74 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3779 74 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3779 74 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3779 74 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3779 74 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL4748908 214035 1 None -6 12 Human 6.2 pKi = 6.2 Binding
GPCRScan assay: inhibition of 5-HT6GPCRScan assay: inhibition of 5-HT6
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
155552826 174092 0 None -37 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 269 3 1 4 2.8 CCn1cncc1-c1c[nH]c2ccc(C(=O)OC)cc12 10.1039/C8MD00313K
CHEMBL4544802 174092 0 None -37 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 269 3 1 4 2.8 CCn1cncc1-c1c[nH]c2ccc(C(=O)OC)cc12 10.1039/C8MD00313K
68108806 131671 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 3 2 5 2.3 CNC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692890 131671 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 3 2 5 2.3 CNC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
11121216 30139 0 None -30 14 Human 7.2 pKi = 7.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 30139 0 None -30 14 Human 7.2 pKi = 7.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
1244725 59490 16 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 417 4 0 6 3.6 CN1CCN(c2oc(-c3ccccc3Cl)nc2S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL1714441 59490 16 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 417 4 0 6 3.6 CN1CCN(c2oc(-c3ccccc3Cl)nc2S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2019.111857
2865 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
59 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
60854 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
CHEMBL708 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
DB00246 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
155555506 174382 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 2 5.1 CN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4552041 174382 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 2 5.1 CN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
126720410 162911 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1F 10.1016/j.ejmech.2017.12.053
CHEMBL4173960 162911 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1F 10.1016/j.ejmech.2017.12.053
2865 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
59 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
60854 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
CHEMBL708 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
DB00246 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
2906559 94413 11 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 316 5 1 6 2.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL251005 94413 11 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 316 5 1 6 2.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
145961959 161495 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4128013 161495 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
5 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
56945045 112061 0 None -7 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 8 1 6 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289956 112061 0 None -7 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 8 1 6 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
71456944 82061 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 486 3 0 4 4.5 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2F)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165564 82061 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 486 3 0 4 4.5 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2F)C1 10.1016/j.bmcl.2012.06.002
25263309 184105 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482568 184105 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
162659577 181358 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4763106 181358 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
44401390 124631 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 223 2 1 1 3.5 Nc1ccc(CC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL364089 124631 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 223 2 1 1 3.5 Nc1ccc(CC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
134134456 143344 0 None -23 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 514 11 1 5 5.4 COc1ccc(-c2cc(F)ccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3897426 143344 0 None -23 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 514 11 1 5 5.4 COc1ccc(-c2cc(F)ccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11849196 80189 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1cccc(N2CCNCC2)c1)c1ccccc1 10.1021/jm060469q
CHEMBL213586 80189 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1cccc(N2CCNCC2)c1)c1ccccc1 10.1021/jm060469q
145953693 162598 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 375 3 1 5 3.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169050 162598 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 375 3 1 5 3.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2017.12.053
118731513 118250 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 477 11 2 6 3.6 NC(=O)c1ccccc1OCCCNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
CHEMBL3409248 118250 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 477 11 2 6 3.6 NC(=O)c1ccccc1OCCCNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
24794436 14069 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL1197511 14069 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL574856 14069 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
10199220 18492 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 266 4 0 4 1.6 CN(C)CCc1cn(S(C)(=O)=O)c2ccccc12 10.1021/jm010943m
CHEMBL127232 18492 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 266 4 0 4 1.6 CN(C)CCc1cn(S(C)(=O)=O)c2ccccc12 10.1021/jm010943m
216239 23795 118 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23795 118 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23795 118 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
5323 202789 103 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
CHEMBL62193 202789 103 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
145983390 165919 0 None -204 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1ccnc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250274 165919 0 None -204 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1ccnc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
155522563 176656 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4453687 176656 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598088 176656 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
71450247 82976 0 None -1258 8 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT6 by Cerep protocol based assayBinding affinity to human 5HT6 by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 82976 0 None -1258 8 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT6 by Cerep protocol based assayBinding affinity to human 5HT6 by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
145977256 163549 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 391 4 1 3 3.5 O=C1Nc2ccccc2C12CCN(CCN1CC=C(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4202947 163549 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 391 4 1 3 3.5 O=C1Nc2ccccc2C12CCN(CCN1CC=C(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
122186880 122980 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 122980 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44389999 13913 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1196367 13913 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL556760 13913 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
10269916 16875 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 360 6 0 4 2.9 COc1ccc2c(c1)C(CCN(C)C)CN2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL124971 16875 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 360 6 0 4 2.9 COc1ccc2c(c1)C(CCN(C)C)CN2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL5275931 193877 0 None 26 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 629 10 0 8 5.4 O=C1CC2CCc3ccsc3C2=NN1CCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
72197845 89844 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL2377590 89844 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
72197845 89844 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
CHEMBL2377590 89844 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
66801000 112062 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 472 7 1 7 4.0 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289957 112062 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 472 7 1 7 4.0 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
10500364 202868 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 386 5 1 6 2.1 COc1ccc(NS(=O)(=O)c2cccc(C#N)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62594 202868 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 386 5 1 6 2.1 COc1ccc(NS(=O)(=O)c2cccc(C#N)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10637020 67640 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2cccc3[nH]ccc23)cc1 10.1021/jm050247c
CHEMBL190521 67640 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2cccc3[nH]ccc23)cc1 10.1021/jm050247c
44398455 67648 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 5 4.6 Cc1c(S(=O)(=O)Nc2cccc3c2ccn3CCN)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL190594 67648 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 5 4.6 Cc1c(S(=O)(=O)Nc2cccc3c2ccn3CCN)sc2ccc(Cl)cc12 10.1021/jm050247c
162662361 181472 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4764557 181472 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
2865 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4143 73 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
23653130 56698 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 463 6 0 7 3.7 CCN1CCN(c2cn(S(=O)(=O)c3cc(OC)ccc3OC)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642429 56698 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 463 6 0 7 3.7 CCN1CCN(c2cn(S(=O)(=O)c3cc(OC)ccc3OC)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
235964 124023 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 263 3 3 4 1.7 Nc1ccc(S(=O)(=O)Nc2cccc(N)c2)cc1 10.1021/jm050247c
CHEMBL362984 124023 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 263 3 3 4 1.7 Nc1ccc(S(=O)(=O)Nc2cccc(N)c2)cc1 10.1021/jm050247c
23625925 93571 0 None -295 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
CHEMBL246484 93571 0 None -295 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
44441238 93712 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 2 1 4 2.0 Nc1cccc2c1OCCN2S(=O)(=O)c1ccccc1F 10.1016/j.bmcl.2006.12.093
CHEMBL247119 93712 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 2 1 4 2.0 Nc1cccc2c1OCCN2S(=O)(=O)c1ccccc1F 10.1016/j.bmcl.2006.12.093
3233 3512 44 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3512 44 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3512 44 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3512 44 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3512 44 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
142601335 186421 0 None -52 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 186421 0 None -52 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
21514234 168541 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2004.01.071
CHEMBL435534 168541 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2004.01.071
68342091 127970 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 6 4.0 COCCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664795 127970 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 6 4.0 COCCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
137637698 155820 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4059916 155820 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
137651330 157478 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
CHEMBL4079397 157478 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
137659459 159131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 5 3.2 Cc1ccc(C)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4097882 159131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 5 3.2 Cc1ccc(C)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
137662033 159151 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(F)cccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4098120 159151 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(F)cccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
22662986 85294 54 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 161 2 2 2 1.1 NCCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260372 85294 54 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 161 2 2 2 1.1 NCCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
44263497 200004 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 4 1 6 4.2 COc1cc2c(cc1NS(=O)(=O)c1c(Cl)nc3sccn13)C(C)=C(C)C2 10.1016/j.bmc.2009.08.006
CHEMBL595301 200004 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 4 1 6 4.2 COc1cc2c(cc1NS(=O)(=O)c1c(Cl)nc3sccn13)C(C)=C(C)C2 10.1016/j.bmc.2009.08.006
24784321 191009 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1ccc(F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518670 191009 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1ccc(F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
57403837 71473 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71473 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71473 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
68115859 132267 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2ccnc2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696980 132267 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2ccnc2)c2oc3c(c2c1)CNCC3 nan
11269402 60537 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3cccc4ccccc34)cccc21 10.1021/jm049615n
CHEMBL175819 60537 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3cccc4ccccc34)cccc21 10.1021/jm049615n
44397420 13005 33 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL1189727 13005 33 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL539327 13005 33 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
6476992 69478 8 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 219 1 1 1 3.8 Nc1ccc(/C=C2\C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL193376 69478 8 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 219 1 1 1 3.8 Nc1ccc(/C=C2\C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
134157171 153938 0 None -99 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 1 6 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccc(OC)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3983496 153938 0 None -99 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 1 6 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccc(OC)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
137645501 157645 0 None -16 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4081383 157645 0 None -16 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
2870750 117930 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 442 4 1 5 6.0 Nc1c(S(=O)(=O)c2ccccc2)sc2nc(-c3ccccc3)cc(-c3ccccc3)c12 10.1016/j.bmcl.2015.03.049
CHEMBL3403334 117930 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 442 4 1 5 6.0 Nc1c(S(=O)(=O)c2ccccc2)sc2nc(-c3ccccc3)cc(-c3ccccc3)c12 10.1016/j.bmcl.2015.03.049
145983128 165825 0 None -128 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248597 165825 0 None -128 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
127037681 136614 0 None -33 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 406 8 1 6 2.4 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cnn(C)c2)CC1 10.1039/C5MD00166H
CHEMBL3739745 136614 0 None -33 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 406 8 1 6 2.4 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cnn(C)c2)CC1 10.1039/C5MD00166H
68108546 131684 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 295 3 1 4 3.9 COc1cc(Oc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692903 131684 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 295 3 1 4 3.9 COc1cc(Oc2ccccc2)cc2c3c(oc12)CCNC3 nan
139488518 169997 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cccc(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4442337 169997 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cccc(F)c12 10.1016/j.ejmech.2019.03.017
44278114 100205 0 None -954 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28833 100205 0 None -954 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
164612518 185394 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4860719 185394 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
5 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
180 401 56 None -99 40 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 56 None -99 40 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 56 None -99 40 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 56 None -99 40 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 56 None -99 40 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
53326048 60131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642869 60131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739584 60131 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
162648765 179760 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4744372 179760 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
162654919 180564 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 603 14 2 8 4.2 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4754024 180564 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 603 14 2 8 4.2 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
155534040 171930 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4470226 171930 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
57391669 71562 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949677 71562 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963079 71562 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
90656155 110826 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 2 4.0 Clc1ccccc1C1CCN(c2ccc3c(c2)CCNCC3)C1 10.1016/j.bmcl.2014.03.049
CHEMBL3260787 110826 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 2 4.0 Clc1ccccc1C1CCN(c2ccc3c(c2)CCNCC3)C1 10.1016/j.bmcl.2014.03.049
22425072 117940 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 457 5 0 4 6.5 Cc1ccc(S(=O)(=O)c2cnc3ccc(F)cc3c2SCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403343 117940 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 457 5 0 4 6.5 Cc1ccc(S(=O)(=O)c2cnc3ccc(F)cc3c2SCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.03.049
4211 57822 83 None 1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57822 83 None 1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
134137560 142705 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3892201 142705 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
117209962 184869 1 None -25 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184869 1 None -25 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
57391158 71557 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949979 71557 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963033 71557 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
145975905 163828 0 None -66 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4206366 163828 0 None -66 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
16118929 60156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642860 60156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739698 60156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
24763353 62625 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783603 62625 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
66801271 112105 0 None -74 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289999 112105 0 None -74 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
68115698 131734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692953 131734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
45488139 196947 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
CHEMBL566410 196947 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
168282733 191059 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 386 9 3 9 1.4 COc1ccccc1N1CCN(CCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5187317 191059 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 386 9 3 9 1.4 COc1ccccc1N1CCN(CCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
66801528 156843 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4071451 156843 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155569568 176194 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 380 7 2 3 5.4 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(Cl)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4593671 176194 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 380 7 2 3 5.4 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(Cl)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
118654425 190577 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5180275 190577 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
2948971 73211 9 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL2011865 73211 9 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
155562202 175818 0 None -67 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4584719 175818 0 None -67 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
137649997 157289 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076903 157289 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
44567985 192395 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL520777 192395 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL5285645 194307 0 None 75 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 629 11 0 8 5.4 O=C1CC2Cc3ccsc3C2=NN1CCCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
162656667 180858 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 589 13 2 8 3.8 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4757296 180858 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 589 13 2 8 3.8 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
46880530 6298 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 402 4 0 5 3.9 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCN(C)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081792 6298 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 402 4 0 5 3.9 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCN(C)C1 10.1016/j.bmcl.2010.01.073
118724637 120614 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360997 120614 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546115 120614 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57391567 71537 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71537 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71537 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
52915868 60985 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762570 60985 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
52915868 60985 6 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762570 60985 6 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
168293874 192179 0 None -15 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192179 0 None -15 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
118731512 118249 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 427 11 2 4 4.4 NC(=O)c1ccccc1OCCCNCCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
CHEMBL3409247 118249 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 427 11 2 4 4.4 NC(=O)c1ccccc1OCCCNCCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
66801229 112057 0 None -758 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289952 112057 0 None -758 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
155554325 176521 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4548353 176521 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4597000 176521 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
155552641 174141 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 3 1 6 5.0 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4546365 174141 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 3 1 6 5.0 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
127036932 137348 0 None -2 22 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 137348 0 None -2 22 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
155562652 175161 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 552 9 1 7 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccc(OC)cc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
CHEMBL4570209 175161 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 552 9 1 7 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccc(OC)cc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
130442572 171908 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171908 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
155537034 172285 0 None -1148 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 240 2 2 3 1.7 Cn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1039/C8MD00313K
CHEMBL4474827 172285 0 None -1148 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 240 2 2 3 1.7 Cn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1039/C8MD00313K
138691338 163667 0 None -229 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 241 3 1 3 3.1 CCn1cncc1-c1c[nH]c2ccc(OC)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4204595 163667 0 None -229 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 241 3 1 3 3.1 CCn1cncc1-c1c[nH]c2ccc(OC)cc12 10.1016/j.ejmech.2019.03.017
155522511 170727 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1OC 10.1016/j.ejmech.2019.111857
CHEMBL4452149 170727 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1OC 10.1016/j.ejmech.2019.111857
164615243 185210 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4857676 185210 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
168288135 191748 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.5 Clc1cccc(Cn2ccc3c(NCC4CCCO4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5197407 191748 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.5 Clc1cccc(Cn2ccc3c(NCC4CCCO4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
752521 198737 8 None -33 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 198737 8 None -33 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
155528967 171392 0 None -15 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 510 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
CHEMBL4462139 171392 0 None -15 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 510 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
44388944 63018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178767 63018 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
155540062 172909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 339 4 2 7 1.3 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)N(C)NC3)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4516220 172909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 339 4 2 7 1.3 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)N(C)NC3)CC1 10.1016/j.ejmech.2019.111857
67003550 192700 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constant
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1CN1CCN(C)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219467 192700 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constant
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1CN1CCN(C)CC1 10.1016/j.bmcl.2021.128275
155557760 174651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4558433 174651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
155531065 171613 0 None 24 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 3 3 4.5 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4465414 171613 0 None 24 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 3 3 4.5 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
90469185 185561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 4 1 7 2.8 COc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
CHEMBL4863272 185561 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 4 1 7 2.8 COc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
90109808 182365 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 325 3 1 3 3.8 Clc1cccc(Cn2ccc3c(N4CCNCC4)cccc32)c1 10.1016/j.ejmech.2020.112765
CHEMBL4784859 182365 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 325 3 1 3 3.8 Clc1cccc(Cn2ccc3c(N4CCNCC4)cccc32)c1 10.1016/j.ejmech.2020.112765
164616626 184552 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 582 13 2 7 6.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4848231 184552 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 582 13 2 7 6.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
126720394 162314 0 None 63 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164541 162314 0 None 63 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
44403093 71438 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196094 71438 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10177537 124376 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363843 124376 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403089 133629 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL371469 133629 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403065 166312 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL427184 166312 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
164615124 185002 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2021.113792
CHEMBL4854568 185002 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2021.113792
44405348 141304 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL383354 141304 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
23655467 89390 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
CHEMBL236988 89390 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
23655469 89392 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236990 89392 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
127046817 139599 0 None 28 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 437 5 0 7 3.2 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C#N)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797435 139599 0 None 28 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 437 5 0 7 3.2 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C#N)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
127047537 139907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 508 4 0 7 3.8 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCOCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3799448 139907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 508 4 0 7 3.8 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCOCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
135398745 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
47 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
CHEMBL715 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
DB00334 2914 112 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
11441983 201789 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606818 201789 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
73453 29616 24 None -10 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29616 24 None -10 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
58258793 127934 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 2 1 4 4.0 Cc1cccc(S(=O)(=O)c2cc(C)c3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664758 127934 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 2 1 4 4.0 Cc1cccc(S(=O)(=O)c2cc(C)c3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258791 128991 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128991 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44240753 139110 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786693 139110 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
46880606 5973 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1079976 5973 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
24783294 176712 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
CHEMBL459987 176712 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
66801346 112099 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289993 112099 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
6918601 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm5003952
CHEMBL127411 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm5003952
58258835 128965 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc2ccccc2n1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
CHEMBL3669642 128965 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc2ccccc2n1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
6918601 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
CHEMBL127411 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
6918601 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL127411 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1016/j.bmcl.2012.06.002
44327527 108492 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 2 2 5 2.1 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N)C3)cc1 10.1021/jm030030n
CHEMBL319956 108492 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 2 2 5 2.1 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N)C3)cc1 10.1021/jm030030n
59339335 139006 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785626 139006 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56593934 65695 0 None 2630 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65695 0 None 2630 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
52913218 70762 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950763 70762 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11317551 60490 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 477 12 2 3 6.6 CCCCN(CCCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL175529 60490 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 477 12 2 3 6.6 CCCCN(CCCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
9999118 6169 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081094 6169 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
71151953 118244 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 542 9 1 5 6.2 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409242 118244 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 542 9 1 5 6.2 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
12017572 204873 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3c(OC)cccc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL75758 204873 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3c(OC)cccc32)c1 10.1016/s0960-894x(00)00453-4
68115749 132269 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 132269 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
58258756 127957 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127957 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
66852770 158870 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4095054 158870 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
16222651 82055 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 474 4 0 4 5.2 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165558 82055 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 474 4 0 4 5.2 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
44537940 18774 0 None 18 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18774 0 None 18 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
68108970 131687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 2 1 2 4.9 CC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692906 131687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 2 1 2 4.9 CC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
134551 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
44435630 89676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL237593 89676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
162651486 180269 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4750587 180269 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
44386822 165986 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 449 5 0 6 4.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3cccnc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL425328 165986 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 449 5 0 6 4.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3cccnc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44435630 89676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL237593 89676 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
71502631 118262 0 None 38 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 475 8 0 6 4.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409260 118262 0 None 38 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 475 8 0 6 4.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
57414666 131721 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1ccc(C(O)C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692940 131721 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1ccc(C(O)C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115687 131745 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692964 131745 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58149663 127422 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659969 127422 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
57391729 69746 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69746 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
58149665 82344 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172183 82344 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
68115874 132257 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 5 2 6 2.7 CC(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696970 132257 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 5 2 6 2.7 CC(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL5088232 215146 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc3ccccc3c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
25024926 62963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785067 62963 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
137630441 161064 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4083893 161064 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116632 161064 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
52912973 70749 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950750 70749 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
57394331 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 nan
CHEMBL1950751 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 nan
44397392 11775 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1181693 11775 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL188864 11775 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
137653219 158658 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 449 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/acs.jmedchem.6b01662
CHEMBL4092681 158658 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 449 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/acs.jmedchem.6b01662
137656608 159609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103281 159609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
57394331 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
CHEMBL1950751 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
49836715 18662 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277010 18662 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
53322548 56687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642418 56687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
24775945 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmc.2023.117256
CHEMBL2220318 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmc.2023.117256
CHEMBL3216565 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmc.2023.117256
24775945 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL2220318 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL3216565 84524 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
9906059 208190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cellsBinding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL98404 208190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cellsBinding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
9908552 18587 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc(Cl)c1 10.1021/jm010943m
CHEMBL127636 18587 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc(Cl)c1 10.1021/jm010943m
9906059 208190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL98404 208190 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
56595402 65637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834226 65637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595402 65637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65637 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595671 65678 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834333 65678 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56593797 65687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834341 65687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
25263297 184337 0 None 19 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 184337 0 None 19 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
24776044 84038 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207389 84038 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
17940234 119999 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccc(C)cc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL350026 119999 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccc(C)cc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9827562 131440 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2cc(Cl)cc(Cl)c2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL369071 131440 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2cc(Cl)cc(Cl)c2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
6918601 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm050247c
CHEMBL127411 18523 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm050247c
134137152 143065 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3895173 143065 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@H]1CCO 10.1016/j.bmc.2016.10.010
46889919 7201 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 3 1 4 2.2 Cn1ccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085618 7201 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 3 1 4 2.2 Cn1ccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
17978406 71441 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196103 71441 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
44403277 166219 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)ccnc12 10.1016/j.bmcl.2005.06.107
CHEMBL426640 166219 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)ccnc12 10.1016/j.bmcl.2005.06.107
135398737 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
135398745 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
17961003 93670 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 3 1 5 3.1 CC(C)(C)c1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246916 93670 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 3 1 5 3.1 CC(C)(C)c1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
44425719 86350 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 483 6 2 4 5.7 CC(C)Nc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231350 86350 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 483 6 2 4 5.7 CC(C)Nc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
44425702 86439 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 444 4 1 3 5.0 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(F)c(Cl)c4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231431 86439 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 444 4 1 3 5.0 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(F)c(Cl)c4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
16222965 82025 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)cc(F)c3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165529 82025 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)cc(F)c3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
46884709 8080 4 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 8080 4 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
46884709 8080 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091208 8080 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
58258773 128989 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OC(F)(F)F)c31)C1CCC(C2)N1 nan
CHEMBL3669666 128989 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OC(F)(F)F)c31)C1CCC(C2)N1 nan
5 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
5202 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
CHEMBL39 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
DB08839 139 72 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
145 140 49 None -7 30 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
1832 140 49 None -7 30 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
CHEMBL7257 140 49 None -7 30 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
DB14010 140 49 None -7 30 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
1150 3878 121 None -7 25 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
125 3878 121 None -7 25 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
CHEMBL6640 3878 121 None -7 25 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
DB08653 3878 121 None -7 25 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
11849794 161883 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/jm060469q
CHEMBL415046 161883 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/jm060469q
164608791 184379 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 515 8 1 6 4.1 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4845699 184379 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 515 8 1 6 4.1 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
164618761 185608 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 9 1 6 3.5 CC(=O)Oc1ccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4863967 185608 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 9 1 6 3.5 CC(=O)Oc1ccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
11849794 161883 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL415046 161883 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/acs.jmedchem.7b00085
90656158 110829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 320 3 1 2 3.7 O=C1CC(c2ccccc2)CN1c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260790 110829 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 320 3 1 2 3.7 O=C1CC(c2ccccc2)CN1c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
45483628 198411 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 440 4 3 8 1.5 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N\NC3=NCCN3)CC4)cc21 10.1021/jm900796p
CHEMBL576967 198411 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 440 4 3 8 1.5 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N\NC3=NCCN3)CC4)cc21 10.1021/jm900796p
56944473 112128 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 488 8 1 7 4.5 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3290021 112128 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 488 8 1 7 4.5 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
71456943 82060 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 534 3 0 4 5.7 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165563 82060 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 534 3 0 4 5.7 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)C1 10.1016/j.bmcl.2012.06.002
25263312 184651 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484965 184651 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
134156305 154249 0 None -36 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3986254 154249 0 None -36 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
164623281 185812 0 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 447 7 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4867109 185812 0 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 447 7 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
2585 803 103 None -109 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 103 None -109 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 103 None -109 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 103 None -109 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 103 None -109 21 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1548953 207679 27 None -3 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 207679 27 None -3 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
155545625 173461 0 None -102 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 255 4 1 3 3.5 CCOc1ccc2[nH]cc(-c3cncn3CC)c2c1 10.1016/j.ejmech.2019.03.017
CHEMBL4529615 173461 0 None -102 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 255 4 1 3 3.5 CCOc1ccc2[nH]cc(-c3cncn3CC)c2c1 10.1016/j.ejmech.2019.03.017
164619936 186209 0 None -1174 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 415 7 0 7 1.6 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4873100 186209 0 None -1174 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 415 7 0 7 1.6 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
16362 3125 71 None -173 30 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
2172 3125 71 None -173 30 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
90 3125 71 None -173 30 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
CHEMBL1423 3125 71 None -173 30 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
DB01100 3125 71 None -173 30 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
155524228 170875 0 None -21 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(F)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4454176 170875 0 None -21 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(F)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
155548205 173750 0 None -2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4536834 173750 0 None -2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
56943891 112051 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289946 112051 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
56593933 65694 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
CHEMBL1834349 65694 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
155546190 176485 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4530770 176485 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596654 176485 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
19958494 99453 1 None -208 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL283036 99453 1 None -208 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
145963649 161522 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4128338 161522 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
117209911 186329 1 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 186329 1 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
162656041 180724 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4755749 180724 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
11508173 94558 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 2 1 3 3.5 CN(C)c1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL251861 94558 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 2 1 3 3.5 CN(C)c1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
118626045 165668 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4244691 165668 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
155514217 169832 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 461 8 0 5 3.9 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4439795 169832 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 461 8 0 5 3.9 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
155551685 175132 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 495 8 0 5 4.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4569757 175132 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 495 8 0 5 4.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
46880706 6085 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(Cl)ccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080694 6085 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(Cl)ccc12 10.1016/j.bmcl.2010.01.073
24784824 176789 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 4 0 6 4.5 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460625 176789 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 4 0 6 4.5 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
1809 134 32 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 32 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 32 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
2948971 73211 9 None 3 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL2011865 73211 9 None 3 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
146025727 171685 0 None -269 27 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171685 0 None -269 27 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
134137732 147769 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3932551 147769 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155541072 172964 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 290 3 2 4 1.7 CCn1cncc1-c1c[nH]c2ccc(S(N)(=O)=O)cc12 10.1039/C8MD00313K
CHEMBL4517552 172964 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 290 3 2 4 1.7 CCn1cncc1-c1c[nH]c2ccc(S(N)(=O)=O)cc12 10.1039/C8MD00313K
155561995 175722 0 None -23 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4582567 175722 0 None -23 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
11515129 155606 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 3 1 4 2.8 COc1cc2c(c(OC)c1)C(=O)C(C)(c1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.11.045
CHEMBL404552 155606 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 3 1 4 2.8 COc1cc2c(c(OC)c1)C(=O)C(C)(c1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.11.045
10251906 2743 18 None -588 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
13550 2743 18 None -588 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
CHEMBL1908863 2743 18 None -588 8 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 IC1=CC(=C(C=C1OC)CCNCC2=C(C=CC=C2)OC)OC 10.1016/j.bmc.2008.04.050
168283351 190796 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 427 4 1 6 4.3 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCOC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
CHEMBL5183690 190796 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 427 4 1 6 4.3 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCOC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
164624803 186212 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873127 186212 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
11703226 94557 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 2 1 3 3.6 COc1cc(Br)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL251857 94557 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 2 1 3 3.6 COc1cc(Br)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
71453361 84424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2163739 84424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219947 84424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
136118661 76257 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 76257 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
10314060 168600 0 None -5248 7 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 168600 0 None -5248 7 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
155565292 175594 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4579883 175594 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
127026052 137553 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137553 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
11258709 130524 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.3 CN(C)CCn1ccc2ccc(NS(=O)(=O)CCc3cccc4ccccc34)cc21 10.1021/jm049615n
CHEMBL368069 130524 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.3 CN(C)CCn1ccc2ccc(NS(=O)(=O)CCc3cccc4ccccc34)cc21 10.1021/jm049615n
11259180 60554 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 6 1 7 3.7 Cc1cc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL175906 60554 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 6 1 7 3.7 Cc1cc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2n1CCN(C)C 10.1021/jm049615n
44401621 68656 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 273 2 1 3 2.7 Nc1ccc(S(=O)(=O)C2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL191972 68656 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 273 2 1 3 2.7 Nc1ccc(S(=O)(=O)C2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL5091373 215567 0 None -354 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 215567 0 None -354 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
168278046 190222 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 401 5 0 5 4.9 COc1cccc(Cn2ccc3c(N4CCC(OC)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5174789 190222 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 401 5 0 5 4.9 COc1cccc(Cn2ccc3c(N4CCC(OC)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
49781036 17183 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 797 17 3 9 8.0 Cc1c(S(=O)(=O)Nc2ccc(OCCCCCCCCNS(=O)(=O)c3cccc4c(N(C)C)cccc34)c(N3CCNCC3)c2)sc2ccc(Cl)cc12 10.1021/jm1007177
CHEMBL1256255 17183 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 797 17 3 9 8.0 Cc1c(S(=O)(=O)Nc2ccc(OCCCCCCCCNS(=O)(=O)c3cccc4c(N(C)C)cccc34)c(N3CCNCC3)c2)sc2ccc(Cl)cc12 10.1021/jm1007177
127036186 137414 0 None -23 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 137414 0 None -23 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
135464118 93060 0 None -21 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 93060 0 None -21 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
3117 207841 103 None -5 16 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -5 16 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
134141166 146757 0 None -93 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 496 11 1 5 5.2 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3924375 146757 0 None -93 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 496 11 1 5 5.2 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
90654848 112697 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233673 112697 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304318 112697 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
52912979 127902 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127902 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
49781032 17181 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 755 13 2 9 6.5 COc1ccc(N(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256253 17181 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 755 13 2 9 6.5 COc1ccc(N(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
9566 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
95882507 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
CHEMBL4520293 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
9566 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
95882507 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
CHEMBL4520293 3426 14 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
851853 191318 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 239 1 1 2 1.5 NC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5191370 191318 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 239 1 1 2 1.5 NC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
5 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
5202 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
CHEMBL39 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
DB08839 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
117209965 185247 1 None -3 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 185247 1 None -3 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
134 2514 24 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2514 24 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2514 24 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2514 24 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2514 24 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
164620074 185679 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 413 8 2 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCNC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4865076 185679 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 413 8 2 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCNC3)cccc21 10.1016/j.ejmech.2021.113792
24966733 84032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207383 84032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
45378936 199506 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 199506 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
57391622 71567 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949970 71567 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963100 71567 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
2351 3286 64 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
2820 3286 64 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
5035 3286 64 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
CHEMBL81 3286 64 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
DB00481 3286 64 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
136118658 76254 0 None -8 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 76254 0 None -8 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
162644502 181806 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 348 4 0 3 3.5 O=C1c2ccccc2/C=C\c2ccccc2N1CCCN1CCOCC1 10.1016/j.bmcl.2020.127493
CHEMBL4778076 181806 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 348 4 0 3 3.5 O=C1c2ccccc2/C=C\c2ccccc2N1CCCN1CCOCC1 10.1016/j.bmcl.2020.127493
137656918 159665 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 372 2 0 5 4.3 N#CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4103891 159665 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 372 2 0 5 4.3 N#CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
90468604 186544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 252 1 2 3 2.1 c1ccc2c(c1)nc(N1CCNCC1)c1cc[nH]c12 10.1021/acs.jmedchem.1c00224
CHEMBL4877935 186544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 252 1 2 3 2.1 c1ccc2c(c1)nc(N1CCNCC1)c1cc[nH]c12 10.1021/acs.jmedchem.1c00224
155561865 175820 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 412 4 2 5 3.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4584746 175820 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 412 4 2 5 3.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
2865 4143 73 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 4143 73 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 4143 73 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 4143 73 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 4143 73 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
155530779 171570 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4464881 171570 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)c1 10.1016/j.ejmech.2019.111857
45487140 198833 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583677 198833 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
68115767 131739 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 0 5 3.7 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(C1COC1)CC3 nan
CHEMBL3692958 131739 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 0 5 3.7 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(C1COC1)CC3 nan
54581122 62542 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782367 62542 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
162672516 183122 0 None -14 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4794963 183122 0 None -14 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
118626101 165724 0 None -251 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245997 165724 0 None -251 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
44389024 63277 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 318 5 1 4 3.0 CCCCS(=O)(=O)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179232 63277 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 318 5 1 4 3.0 CCCCS(=O)(=O)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
145983144 165880 0 None -7 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249426 165880 0 None -7 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
162662778 181992 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 552 10 1 5 6.1 C#CCNC1CCc2c(OCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4780446 181992 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 552 10 1 5 6.1 C#CCNC1CCc2c(OCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
11567840 94844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 413 1 2 3 4.6 CC1(c2ccc(O)c(Br)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253718 94844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 413 1 2 3 4.6 CC1(c2ccc(O)c(Br)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
168288598 191773 0 None -1949 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 400 10 3 9 1.8 COc1ccccc1N1CCN(CCCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5197911 191773 0 None -1949 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 400 10 3 9 1.8 COc1ccccc1N1CCN(CCCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
1209 1658 75 None -12 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1658 75 None -12 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1658 75 None -12 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1658 75 None -12 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1658 75 None -12 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
168287240 191737 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 7 4.4 Nc1nc(NCCOc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5197266 191737 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 7 4.4 Nc1nc(NCCOc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
156012823 177410 0 None -29 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 548 11 0 6 6.2 Cc1ccc(S(=O)(=O)N(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2ccccc2)cc1 10.1016/j.bmc.2020.115459
CHEMBL4638388 177410 0 None -29 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 548 11 0 6 6.2 Cc1ccc(S(=O)(=O)N(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2ccccc2)cc1 10.1016/j.bmc.2020.115459
4976400 173702 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 361 7 2 4 4.7 O=[N+]([O-])c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4535764 173702 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 361 7 2 4 4.7 O=[N+]([O-])c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
145978472 163603 0 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 438 4 1 4 2.7 O=C(c1ccc(Cl)cc1)N1CCN(CCN2CCC3(C2)C(=O)Nc2ccccc23)CC1 10.1016/j.bmcl.2018.06.019
CHEMBL4203581 163603 0 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 438 4 1 4 2.7 O=C(c1ccc(Cl)cc1)N1CCN(CCN2CCC3(C2)C(=O)Nc2ccccc23)CC1 10.1016/j.bmcl.2018.06.019
124 2981 47 None -100 33 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 47 None -100 33 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 47 None -100 33 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 47 None -100 33 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 47 None -100 33 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
206 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
68848 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
CHEMBL12314 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
206 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
68848 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
CHEMBL12314 2493 16 None -1318 25 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
138691364 171907 2 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 254 3 2 3 2.2 CCn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4469847 171907 2 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 254 3 2 3 2.2 CCn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1016/j.ejmech.2019.03.017
155554326 174948 0 None -99 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4565558 174948 0 None -99 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
58258770 127960 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ncccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664785 127960 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ncccc54)ccc31)C1CCC(C2)N1 nan
5 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
5202 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
CHEMBL39 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
DB08839 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
145 140 49 None -7 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
1832 140 49 None -7 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
CHEMBL7257 140 49 None -7 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
DB14010 140 49 None -7 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
54585045 62537 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782362 62537 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
155524885 176221 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4455699 176221 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4594629 176221 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
102 4127 48 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4127 48 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4127 48 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4127 48 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4127 48 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
2133793 21817 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 476 5 2 5 6.2 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccc(F)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL1319488 21817 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 476 5 2 5 6.2 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccc(F)cc1 10.1016/j.bmcl.2015.03.049
155532545 171752 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 380 4 2 5 3.2 CC(=O)Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4467359 171752 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 380 4 2 5 3.2 CC(=O)Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
44591069 176717 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 461 4 0 6 4.9 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460002 176717 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 461 4 0 6 4.9 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
44328589 207694 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCN(C)CC4)cc3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95517 207694 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCN(C)CC4)cc3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10811310 102200 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL302845 102200 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10436045 3516 4 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3516 4 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3516 4 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
44398420 67875 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCNCC4)cc3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL191027 67875 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCNCC4)cc3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
10811310 102200 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm050247c
CHEMBL302845 102200 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm050247c
134131970 144927 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 487 8 1 5 4.7 CC(=O)Nc1ccc(CCN(C)CC2Cc3ccc4c(ccn4S(=O)(=O)c4ccccc4)c32)cc1 10.1016/j.bmc.2016.10.010
CHEMBL3910287 144927 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 487 8 1 5 4.7 CC(=O)Nc1ccc(CCN(C)CC2Cc3ccc4c(ccn4S(=O)(=O)c4ccccc4)c32)cc1 10.1016/j.bmc.2016.10.010
145973771 164719 0 None -9 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 164719 0 None -9 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
130442480 175270 0 None -97 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 175270 0 None -97 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
137631892 156385 0 None -15 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4066426 156385 0 None -15 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
58258864 127938 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 1 6 2.5 Cc1cc(S(=O)(=O)c2cncnc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664762 127938 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 1 6 2.5 Cc1cc(S(=O)(=O)c2cncnc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
155556527 174510 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 247 2 1 2 3.3 CCn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4555115 174510 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 247 2 1 2 3.3 CCn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
155566925 175864 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 293 1 1 2 3.5 Cn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4585956 175864 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 293 1 1 2 3.5 Cn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
10808841 203290 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 365 5 1 7 1.0 COc1ccc(NS(=O)(=O)c2cn(C)cn2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL64715 203290 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 365 5 1 7 1.0 COc1ccc(NS(=O)(=O)c2cn(C)cn2)cc1N1CCN(C)CC1 10.1021/jm980532e
49850567 56469 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632217 56469 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44439165 145753 0 None -3162 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391661 145753 0 None -3162 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
168295497 192502 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5209131 192502 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
9952250 204960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL76466 204960 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1016/s0960-894x(00)00453-4
155555136 174348 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cnc2ccccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4551197 174348 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cnc2ccccc2c1 10.1021/acsmedchemlett.6b00056
164612759 184717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 477 13 2 6 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850488 184717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 477 13 2 6 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
164621427 185790 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 12 2 6 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4866788 185790 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 12 2 6 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
134130197 142219 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 10 1 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884312 142219 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 10 1 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134129897 142241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 11 1 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884704 142241 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 11 1 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130069 142256 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 607 10 1 7 6.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884858 142256 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 607 10 1 7 6.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
56595406 65642 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
CHEMBL1834230 65642 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
2870667 94080 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 2 5 3.3 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
CHEMBL249034 94080 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 2 5 3.3 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
11624561 70287 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL187865 70287 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL194307 70287 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10202995 70553 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194786 70553 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44403096 72128 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
CHEMBL197845 72128 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
11524473 134839 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL371886 134839 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
49781038 17726 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 440 6 2 6 3.1 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1258607 17726 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 440 6 2 6 3.1 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
155534795 176251 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4471055 176251 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594879 176251 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
14571158 149081 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL394303 149081 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
127047538 139755 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 482 6 0 7 3.3 COCCS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798490 139755 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 482 6 0 7 3.3 COCCS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
11200157 201763 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606705 201763 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
11775364 201787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 201787 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
25122654 200528 0 None 54 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 200528 0 None 54 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
58258859 124425 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 384 2 1 4 3.8 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3639636 124425 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 384 2 1 4 3.8 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
20901115 10964 5 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10964 5 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
49836617 18804 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278180 18804 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
25263326 184290 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484009 184290 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
16222963 82043 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165546 82043 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
58258804 127931 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 372 2 0 5 3.8 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccsc4)cc13)C2 nan
CHEMBL3664755 127931 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 372 2 0 5 3.8 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccsc4)cc13)C2 nan
56595534 65648 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
CHEMBL1834238 65648 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
52912973 70749 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70749 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
155547259 173663 0 None 21 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4534733 173663 0 None 21 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
16222450 82050 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 368 3 0 4 3.6 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165553 82050 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 368 3 0 4 3.6 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
9885426 117352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 364 6 0 6 3.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccs1 10.1021/jm010943m
CHEMBL339741 117352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 364 6 0 6 3.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccs1 10.1021/jm010943m
44435623 148997 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394232 148997 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25024529 62959 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
CHEMBL1785063 62959 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
44435623 148997 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL394232 148997 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5080955 214712 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)c(Cl)c1 10.1021/acs.jmedchem.1c00497
CHEMBL5092755 215387 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1ccc(S(=O)(=O)CC2CCN(CCCc3noc4cc(F)ccc34)C2)cc1C 10.1021/acs.jmedchem.1c00497
135398745 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
47 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
CHEMBL715 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
DB00334 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
58230832 177248 2 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 258 1 0 5 1.6 O=S(=O)(Cl)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
CHEMBL4635924 177248 2 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 258 1 0 5 1.6 O=S(=O)(Cl)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
CHEMBL5287809 194396 0 None 218 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 615 10 0 8 5.0 O=C1CC2Cc3ccsc3C2=NN1CCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
58258858 127921 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 388 2 1 4 3.6 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)cc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664745 127921 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 388 2 1 4 3.6 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)cc(F)c4)ccc31)C1CCC(C2)N1 nan
56665086 65686 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834340 65686 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
44403064 133572 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371132 133572 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435607 89137 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236576 89137 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
164610136 184935 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 398 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4853545 184935 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 398 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCC3)cccc21 10.1016/j.ejmech.2021.113792
44435607 89137 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236576 89137 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
162651292 180222 0 None -6 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
CHEMBL4749824 180222 0 None -6 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
24965331 84109 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 477 5 0 6 3.4 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)c(Br)c1 10.1016/j.bmcl.2012.10.057
CHEMBL2207768 84109 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 477 5 0 6 3.4 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)c(Br)c1 10.1016/j.bmcl.2012.10.057
164627753 186507 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 596 14 2 7 6.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4877482 186507 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 596 14 2 7 6.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
23652635 56686 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 411 5 0 5 4.1 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642417 56686 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 411 5 0 5 4.1 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
68115704 131759 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692978 131759 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
59339383 139136 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787014 139136 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
10091613 156726 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4070284 156726 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
47 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
CHEMBL715 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
DB00334 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
137637392 156218 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 6 0 6 3.0 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4064478 156218 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 6 0 6 3.0 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
47 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
CHEMBL715 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
DB00334 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
56944665 112110 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290003 112110 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
68115843 132250 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696963 132250 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
16222448 82019 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165523 82019 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
162646653 179502 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4741142 179502 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
162654406 180580 0 None -22 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4754193 180580 0 None -22 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
162657622 181137 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4760655 181137 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
53327952 111688 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286581 111688 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
58258843 128993 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccn4)c31)C1CCC(C2)N1 nan
CHEMBL3669670 128993 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccn4)c31)C1CCC(C2)N1 nan
49756 204312 13 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 204312 13 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
52899 97254 34 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm030030n
CHEMBL268800 97254 34 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm030030n
CHEMBL5281673 194122 0 None 47 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 643 12 0 8 5.8 O=C1CC2Cc3ccsc3C2=NN1CCCCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
137659244 159168 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
CHEMBL4098336 159168 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
145958329 162332 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4164725 162332 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
145949620 162745 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 383 5 1 5 3.9 CC(C)c1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4171417 162745 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 383 5 1 5 3.9 CC(C)c1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
2854567 153924 9 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 7 1 6 4.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCCOc3ccc(C(C)(C)C)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL398337 153924 9 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 7 1 6 4.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCCOc3ccc(C(C)(C)C)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
44263496 201525 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL605292 201525 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
12017579 99196 14 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(CCN(C)C)c[nH]c2c1 10.1021/jm030030n
CHEMBL281408 99196 14 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(CCN(C)C)c[nH]c2c1 10.1021/jm030030n
156017609 177901 0 None -40 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 464 9 1 6 4.9 O=C1CCc2cc(OCCCCCCN3CCN(c4nsc5ccccc45)CC3)ccc2N1 10.1016/j.bmc.2020.115459
CHEMBL4644906 177901 0 None -40 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 464 9 1 6 4.9 O=C1CCc2cc(OCCCCCCN3CCN(c4nsc5ccccc45)CC3)ccc2N1 10.1016/j.bmc.2020.115459
155540807 172516 0 None -12 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccccc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4483554 172516 0 None -12 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccccc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
54584108 62532 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782357 62532 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
75201901 166425 19 None -602 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 166425 19 None -602 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
90654850 112646 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233674 112646 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302943 112646 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
57403055 70747 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cccc(S(=O)(=O)c4ccccc4)c31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950748 70747 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cccc(S(=O)(=O)c4ccccc4)c31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
155557523 174665 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 433 4 0 6 4.2 COc1ccc2c(c1)c(C1=CCN(C)CC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4558840 174665 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 433 4 0 6 4.2 COc1ccc2c(c1)c(C1=CCN(C)CC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
162661549 181402 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
CHEMBL4763622 181402 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
118626035 165518 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240954 165518 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
23652863 56696 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 5 0 6 3.7 CCN1CCN(c2cn(S(=O)(=O)c3ccc(OC)cc3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642427 56696 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 5 0 6 3.7 CCN1CCN(c2cn(S(=O)(=O)c3ccc(OC)cc3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
11575479 94743 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253096 94743 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
19779451 93746 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 222 2 1 2 3.3 Nc1ccc(Cn2ccc3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247281 93746 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 222 2 1 2 3.3 Nc1ccc(Cn2ccc3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
57399090 68421 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmc.2011.09.044
CHEMBL1917342 68421 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmc.2011.09.044
3397 205488 112 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 205488 112 None - 1 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
137650961 157333 0 None -50 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4077538 157333 0 None -50 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
126720449 162455 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4166780 162455 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
155541547 173038 0 None 22 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 486 8 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4519004 173038 0 None 22 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 486 8 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155563164 175326 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 4 2 5 3.8 CC(=O)Nc1nc(C)c(-c2c(C)n(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4573880 175326 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 4 2 5 3.8 CC(=O)Nc1nc(C)c(-c2c(C)n(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
71151870 118254 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409252 118254 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.12.045
57398613 71468 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949759 71468 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962394 71468 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
66801167 112109 0 None -165 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290002 112109 0 None -165 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
74538690 143064 0 None -23 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 511 10 1 4 5.2 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3895172 143064 0 None -23 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 511 10 1 4 5.2 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
71456780 81419 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 4 3.5 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccc(Cl)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159462 81419 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 4 3.5 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccc(Cl)c1 10.1016/j.ejmech.2012.07.043
44581973 175601 0 None -389 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175601 0 None -389 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
162645470 179544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4741579 179544 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
118736372 118944 0 None -13 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 7 0 9 2.6 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423336 118944 0 None -13 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 7 0 9 2.6 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
168281850 191037 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.3 Clc1cccc(Cn2ccc3c(NCC4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5187034 191037 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.3 Clc1cccc(Cn2ccc3c(NCC4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
164616670 184613 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4849077 184613 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
118736397 118951 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 511 7 0 10 1.7 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423379 118951 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 511 7 0 10 1.7 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
71463516 85296 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 329 5 0 5 2.4 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260374 85296 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 329 5 0 5 2.4 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccncc12 10.1007/s00044-004-0121-8
5 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 72 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
90656159 110830 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 321 3 1 3 2.6 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260791 110830 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 321 3 1 3 2.6 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
50878551 90745 61 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 61 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
66800991 112068 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 8 2.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289963 112068 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 8 2.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
142601333 185763 0 None -36 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185763 0 None -36 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
44404396 71457 0 None -45 5 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196169 71457 0 None -45 5 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
134153716 152484 0 None -70 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3971125 152484 0 None -70 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11849789 166170 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1ccc(N2CCNCC2)cc1)c1ccccc1 10.1021/jm060469q
CHEMBL426332 166170 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1ccc(N2CCNCC2)cc1)c1ccccc1 10.1021/jm060469q
44568065 191086 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 4 0 5 3.7 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C(C)C)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL518762 191086 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 4 0 5 3.7 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C(C)C)CC3)c1 10.1016/j.bmcl.2008.06.030
155562519 175212 0 None -17 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccc(F)cc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4571321 175212 0 None -17 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccc(F)cc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
57391618 71469 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71469 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71469 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57403835 71471 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949767 71471 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962397 71471 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
50878551 90745 61 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 61 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
11407151 61613 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL177119 61613 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2n1CCN(C)C 10.1021/jm049615n
10028436 3532 5 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3532 5 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3532 5 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
6075 150108 42 None -13 16 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 150108 42 None -13 16 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
156015769 177579 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 388 4 1 5 2.8 COc1cc2c3c(c1OC)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640588 177579 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 388 4 1 5 2.8 COc1cc2c3c(c1OC)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
164615243 185210 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4857676 185210 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
118736396 118950 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 6 0 10 1.3 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423378 118950 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 6 0 10 1.3 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
136118649 76322 0 None -9 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058704 76322 0 None -9 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
90654840 112634 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233669 112634 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302757 112634 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
145990586 166843 0 None -67 11 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166843 0 None -67 11 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
55479093 81421 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 366 7 1 5 2.6 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159464 81421 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 366 7 1 5 2.6 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
2291 3184 58 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3184 58 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3184 58 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3184 58 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3184 58 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL5282158 194146 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cell membrane incubated for 60 mins by microplate beta scintillation counting analysis
ChEMBL 657 12 0 8 6.2 O=C1CC2CCc3ccsc3C2=NN1CCCCCCCN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmc.2023.117256
155562918 175183 0 None 5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4570584 175183 0 None 5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
127045870 140088 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 416 5 0 8 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3cnn(C)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800576 140088 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 416 5 0 8 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3cnn(C)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
90656169 110840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 338 3 1 4 3.1 COc1ccccc1C1CN(c2ccc3c(c2)CCNCC3)C(=O)O1 10.1016/j.bmcl.2014.03.049
CHEMBL3260802 110840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 338 3 1 4 3.1 COc1ccccc1C1CN(c2ccc3c(c2)CCNCC3)C(=O)O1 10.1016/j.bmcl.2014.03.049
56944664 112073 0 None -79 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289968 112073 0 None -79 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
7185124 10953 2 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173210 10953 2 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
846090 169589 9 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 286 7 1 5 2.3 Cc1cc(OCCN(C)C)nc(NCc2ccccc2)n1 10.1016/j.ejmech.2019.111857
CHEMBL4436098 169589 9 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 286 7 1 5 2.3 Cc1cc(OCCN(C)C)nc(NCc2ccccc2)n1 10.1016/j.ejmech.2019.111857
44397258 13805 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1195611 13805 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL554985 13805 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
135476741 155525 11 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL404232 155525 11 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
11631738 94651 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 1 1 2 4.7 CC1(c2ccc(Cl)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL252496 94651 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 1 1 2 4.7 CC1(c2ccc(Cl)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
122483275 138110 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 138110 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 138110 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
107 141 121 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
1833 141 121 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
CHEMBL8165 141 121 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
137651282 157455 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccccc3F)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4079150 157455 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccccc3F)n2)CC1 10.1016/j.ejmech.2017.04.033
45484332 197131 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 373 5 0 5 3.1 O=S(=O)(c1cccc(F)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
CHEMBL567805 197131 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 373 5 0 5 3.1 O=S(=O)(c1cccc(F)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
49836507 18748 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
CHEMBL1277835 18748 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
24784578 176716 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 4.7 CCCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL460001 176716 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 4.7 CCCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
16023081 59977 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 356 3 1 5 2.6 COc1cc(OC)cc(N2C(=O)CSC23C(=O)Nc2ccccc23)c1 10.1016/j.bmcl.2014.03.049
CHEMBL1733660 59977 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 356 3 1 5 2.6 COc1cc(OC)cc(N2C(=O)CSC23C(=O)Nc2ccccc23)c1 10.1016/j.bmcl.2014.03.049
71727067 91266 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401937 91266 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3217036 91266 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
25251903 175218 11 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 334 4 0 5 3.2 CN1CCN(c2ccnc(SCc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4571369 175218 11 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 334 4 0 5 3.2 CN1CCN(c2ccnc(SCc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.111857
49756 204312 13 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm010943m
CHEMBL7143 204312 13 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm010943m
44568019 183911 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1cccc(C(F)(F)F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL481278 183911 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1cccc(C(F)(F)F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
242 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
34 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
60795 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL1112 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
DB01238 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL5076846 214464 0 None -138 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccc(F)cc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
44446214 94929 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL254331 94929 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
2883218 174816 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 350 5 1 4 4.8 Oc1c(CN2CCCC2)cc(CSc2ccccc2)c2cccnc12 10.1016/j.ejmech.2019.111857
CHEMBL4562431 174816 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 350 5 1 4 4.8 Oc1c(CN2CCCC2)cc(CSc2ccccc2)c2cccnc12 10.1016/j.ejmech.2019.111857
13069626 120605 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3361000 120605 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546103 120605 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
9923440 114178 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 327 8 2 4 2.9 OCCCNC[C@H]1CCc2ccc(OCc3ccccc3)cc2O1 10.1021/jm5003952
CHEMBL3329448 114178 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 327 8 2 4 2.9 OCCCNC[C@H]1CCc2ccc(OCc3ccccc3)cc2O1 10.1021/jm5003952
58258795 129015 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669692 129015 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
129892069 192741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assayDisplacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assay
ChEMBL 428 6 1 5 4.2 CN(C)CCn1cnc2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc21 10.1016/j.bmcl.2021.128275
CHEMBL5220504 192741 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assayDisplacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assay
ChEMBL 428 6 1 5 4.2 CN(C)CCn1cnc2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc21 10.1016/j.bmcl.2021.128275
155563374 175246 0 None 131 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4572158 175246 0 None 131 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
25131339 181023 0 None 26 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4759208 181023 0 None 26 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
118626121 165420 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238479 165420 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
10117854 127425 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL366012 127425 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
53327952 111688 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286581 111688 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
164623922 186165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 456 8 1 5 5.2 O=S(=O)(c1cccc2ccccc12)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4872486 186165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 456 8 1 5 5.2 O=S(=O)(c1cccc2ccccc12)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
155531362 171627 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 456 6 2 6 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc(F)c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4465638 171627 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 456 6 2 6 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc(F)c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155568300 176374 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4590882 176374 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4595815 176374 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155555526 176404 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4552168 176404 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4596003 176404 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155521504 176595 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4451939 176595 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4597600 176595 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
45484299 197217 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568249 197217 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
155555238 174330 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4550806 174330 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
11154032 202296 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 407 5 3 3 4.1 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1Cl 10.1021/jm049243i
CHEMBL610255 202296 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 407 5 3 3 4.1 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1Cl 10.1021/jm049243i
11201726 202300 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
CHEMBL610259 202300 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
44397650 13764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL1195348 13764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL554369 13764 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
162651619 180311 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4751063 180311 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
71462330 82046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Cl)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165549 82046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Cl)C1 10.1016/j.bmcl.2012.06.002
58258791 128991 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128991 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
66800947 158233 0 None -9 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4088249 158233 0 None -9 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
137638969 156871 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3c(Cl)cccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4071816 156871 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3c(Cl)cccc32)cc1 10.1021/acs.jmedchem.6b01662
137644304 158053 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4085949 158053 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
44403059 124373 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363827 124373 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
11574663 155109 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 390 4 1 3 4.9 CCN(CC)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL401970 155109 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 390 4 1 3 4.9 CCN(CC)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
23652787 56688 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642419 56688 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
58258827 127956 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 467 3 1 5 5.3 Cn1c2c(c3cc(S(=O)(=O)c4cn(-c5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664781 127956 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 467 3 1 5 5.3 Cn1c2c(c3cc(S(=O)(=O)c4cn(-c5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
20042470 13912 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1196366 13912 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL556759 13912 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
56595531 65646 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
CHEMBL1834235 65646 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
25263308 184239 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483560 184239 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
10203612 61624 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 439 8 2 3 5.2 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cc(Cl)cc(Cl)c3)cc12 10.1021/jm049615n
CHEMBL177124 61624 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 439 8 2 3 5.2 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cc(Cl)cc(Cl)c3)cc12 10.1021/jm049615n
68108369 131669 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 6 3.1 O=S(=O)(c1ccccc1)c1cc(-n2cccn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692888 131669 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 6 3.1 O=S(=O)(c1ccccc1)c1cc(-n2cccn2)c2oc3c(c2c1)CNCC3 nan
25024726 62969 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(Cl)cc2)CC1 10.1021/ml100101u
CHEMBL1785073 62969 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(Cl)cc2)CC1 10.1021/ml100101u
44435644 89129 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236571 89129 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44386408 63007 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 5 0 5 4.2 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL178691 63007 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 5 0 5 4.2 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44435644 89129 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236571 89129 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
12017573 163444 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3ccc(OC)cc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL419824 163444 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3ccc(OC)cc32)c1 10.1016/s0960-894x(00)00453-4
135398737 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 958 93 None -4 89 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
16116900 60101 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642847 60101 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739252 60101 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
68115752 132272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 0 4 3.8 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3696985 132272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 0 4 3.8 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
58258841 129011 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669688 129011 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
10091389 158203 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4087957 158203 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
46880657 6379 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082198 6379 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
52912973 70749 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70749 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
24763349 62630 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783608 62630 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
135339817 181484 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 181484 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
11316967 129754 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 453 4 2 3 5.6 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5c(Cl)cccc45)cc23)CC1 10.1021/jm049615n
CHEMBL367481 129754 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 453 4 2 3 5.6 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5c(Cl)cccc45)cc23)CC1 10.1021/jm049615n
24783809 176713 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459988 176713 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
162654006 180490 0 None -39 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
CHEMBL4753094 180490 0 None -39 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
11236269 129305 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
CHEMBL367088 129305 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
9953284 204796 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm010943m
CHEMBL75010 204796 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm010943m
16116898 60128 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1642877 60128 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1739545 60128 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
16117282 60138 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642888 60138 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739615 60138 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
44403046 135260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 3 1 5 3.4 O=S(=O)(c1cccs1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL372569 135260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 3 1 5 3.4 O=S(=O)(c1cccs1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398803 69742 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69742 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69742 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
11236269 129305 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367088 129305 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
68108586 124459 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3639917 124459 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCNC3 nan
24965680 84020 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207371 84020 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
44397322 12255 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1184645 12255 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL361892 12255 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
71151683 118253 0 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(F)c2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409251 118253 0 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(F)c2)CC1 10.1016/j.ejmech.2014.12.045
68115694 131719 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1cc(F)cc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692938 131719 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1cc(F)cc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23955921 109740 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 413 8 1 5 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL322980 109740 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 413 8 1 5 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
155541866 173049 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4519266 173049 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
242 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
34 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
60795 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
CHEMBL1112 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
DB01238 470 124 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
52945114 17172 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 776 17 4 9 6.2 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNC(=O)CCCCC2SC[C@@H]3NC(=O)N[C@H]23)CC1 10.1021/jm1007177
CHEMBL1256172 17172 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 776 17 4 9 6.2 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNC(=O)CCCCC2SC[C@@H]3NC(=O)N[C@H]23)CC1 10.1021/jm1007177
24777062 94691 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
CHEMBL252774 94691 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
24776941 94794 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 5 0 3 4.3 CN(C)CCc1cn(Sc2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL253397 94794 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 5 0 3 4.3 CN(C)CCc1cn(Sc2ccccc2)c2ccccc12 10.1021/jm070910s
11259419 198677 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 1 5 5.2 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL579981 198677 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 1 5 5.2 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
137634238 156652 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 394 4 0 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(C#N)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4069360 156652 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 394 4 0 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(C#N)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
24966738 84030 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207381 84030 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
145954503 162419 0 None 7 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 370 5 1 4 4.1 O[C@H](CCN1CCc2onc(-c3ccc(F)c(F)c3)c2C1)c1ccccc1 10.1016/j.ejmech.2018.04.010
CHEMBL4166092 162419 0 None 7 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 370 5 1 4 4.1 O[C@H](CCN1CCc2onc(-c3ccc(F)c(F)c3)c2C1)c1ccccc1 10.1016/j.ejmech.2018.04.010
71574206 86268 0 None -39 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 512 7 1 5 4.7 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312641 86268 0 None -39 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 512 7 1 5 4.7 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
176 398 66 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
164618482 185915 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4868911 185915 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
1534 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
71458650 81431 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cccc(Cl)c2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159474 81431 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cccc(Cl)c2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
4723431 171423 14 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 316 6 2 2 4.8 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4462814 171423 14 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 316 6 2 2 4.8 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
137633849 156620 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(OC)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4069104 156620 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(OC)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
10246639 6061 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCNCC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080574 6061 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCNCC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
57399547 70751 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 0 4 4.1 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
CHEMBL1950752 70751 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 0 4 4.1 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
155558408 174755 0 None 4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(Cl)ccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4560883 174755 0 None 4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(Cl)ccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
1534 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103040 53 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
118724647 120606 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361004 120606 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546104 120606 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
155552213 176658 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4546775 176658 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598090 176658 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
56944952 157367 0 None -26 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4077937 157367 0 None -26 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
145985505 165625 0 None -30 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243579 165625 0 None -30 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
126720407 162826 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 365 5 1 6 3.0 COc1cccc(Cn2c(C(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172620 162826 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 365 5 1 6 3.0 COc1cccc(Cn2c(C(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
24855831 65635 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 404 5 1 3 3.5 CCC1C=NN(/C(=N/S(=O)(=O)c2ccccc2Cl)NCc2ccccc2)C1 10.1021/jm200466r
CHEMBL1834222 65635 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 404 5 1 3 3.5 CCC1C=NN(/C(=N/S(=O)(=O)c2ccccc2Cl)NCc2ccccc2)C1 10.1021/jm200466r
56593935 65696 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 378 5 1 3 2.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CF)(CF)C=N1 10.1021/jm200466r
CHEMBL1834351 65696 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 378 5 1 3 2.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CF)(CF)C=N1 10.1021/jm200466r
25263316 184412 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 295 4 1 2 4.3 Cc1cccc(COc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484608 184412 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 295 4 1 2 4.3 Cc1cccc(COc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
134131976 144975 0 None -34 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 509 10 1 5 5.2 N#Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccc(F)cc3-c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3910730 144975 0 None -34 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 509 10 1 5 5.2 N#Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccc(F)cc3-c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11603453 155290 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 7 1 4 4.6 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL402923 155290 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 7 1 4 4.6 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12017575 204739 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL74378 204739 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)cc1 10.1016/s0960-894x(00)00453-4
155563827 176440 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4572629 176440 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4596298 176440 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
24763351 62622 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783600 62622 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
5 139 72 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 72 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 72 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 72 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
164620109 185727 0 None -54 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 466 8 0 6 4.4 CN1CCN(Cc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
CHEMBL4865907 185727 0 None -54 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 466 8 0 6 4.4 CN1CCN(Cc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
168291659 192038 0 None -131 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5202120 192038 0 None -131 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
71727065 102409 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401931 102409 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3039720 102409 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
155530351 176284 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4464370 176284 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595115 176284 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
44438723 151572 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 5 0 4 3.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL396329 151572 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 5 0 4 3.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
11417978 63675 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
CHEMBL180110 63675 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
145985718 165525 0 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241081 165525 0 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
121238069 159126 0 None 79 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4097856 159126 0 None 79 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
137630619 161082 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4094296 161082 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4116784 161082 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
164615340 185429 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4861431 185429 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
56944189 112093 0 None -16 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 454 8 1 8 2.4 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289987 112093 0 None -16 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 454 8 1 8 2.4 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
53327953 111690 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286583 111690 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
71455001 81439 0 None -4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 7 1 4 2.5 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159482 81439 0 None -4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 7 1 4 2.5 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155533028 171796 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 458 9 0 5 5.1 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4468036 171796 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 458 9 0 5 5.1 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
11683768 94739 1 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 1 1 2 4.7 CC1(c2ccc(I)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253061 94739 1 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 1 1 2 4.7 CC1(c2ccc(I)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
71449642 81433 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 7 1 5 2.8 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159476 81433 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 7 1 5 2.8 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
10450930 82018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 356 4 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)c1n2S(=O)(=O)c2ccccc2-1 10.1016/j.bmcl.2012.06.002
CHEMBL2165522 82018 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 356 4 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)c1n2S(=O)(=O)c2ccccc2-1 10.1016/j.bmcl.2012.06.002
71456783 81437 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 418 7 1 4 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159480 81437 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 418 7 1 4 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
53327953 111690 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286583 111690 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
137644129 158163 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 545 6 0 6 4.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(OCC(F)(F)F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4087429 158163 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 545 6 0 6 4.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(OCC(F)(F)F)cc23)CC1 10.1021/acs.jmedchem.6b01662
86288949 112625 0 None -245 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233665 112625 0 None -245 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302599 112625 0 None -245 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
168299277 192695 0 None -281 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 404 8 0 5 4.2 CCOCC(Oc1c(C)cccc1Cl)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219333 192695 0 None -281 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 404 8 0 5 4.2 CCOCC(Oc1c(C)cccc1Cl)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
2872937 117928 6 None 2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 464 4 1 5 4.7 O=S(=O)(Nc1cc2c(c3ccccc13)OC1(N3CCOCC3)CCCCC21)c1ccccc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403332 117928 6 None 2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 464 4 1 5 4.7 O=S(=O)(Nc1cc2c(c3ccccc13)OC1(N3CCOCC3)CCCCC21)c1ccccc1 10.1016/j.bmcl.2015.03.049
162672560 183182 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4795614 183182 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
162676389 183380 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4797942 183380 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
127033666 138971 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785278 138971 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
58158748 139093 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786563 139093 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
11476494 78946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 8 1 7 4.1 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
CHEMBL2112986 78946 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 8 1 7 4.1 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
24966734 84033 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 497 4 0 5 4.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207384 84033 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 497 4 0 5 4.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL5079536 214622 0 None -14 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1c(S(=O)(=O)N[C@H]2C[C@H](C)N(CCCc3noc4cc(F)ccc34)C2)sc2ccc(Cl)cc12 10.1021/acs.jmedchem.1c00497
152215 96998 53 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL26655 96998 53 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
10315621 66130 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2c(F)cccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184066 66130 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2c(F)cccc21 10.1016/j.bmcl.2004.09.003
52899 97254 34 None 7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm990550b
CHEMBL268800 97254 34 None 7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm990550b
44405257 73002 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 4 1 8 2.3 Nc1ccc(S(=O)(=O)n2ccc3c([N+](=O)[O-])cc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL200844 73002 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 4 1 8 2.3 Nc1ccc(S(=O)(=O)n2ccc3c([N+](=O)[O-])cc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2005.08.059
118712403 114157 0 None - 1 Human 7.0 pKi = 7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 320 2 1 3 3.8 O=C(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL3329427 114157 0 None - 1 Human 7.0 pKi = 7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 320 2 1 3 3.8 O=C(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
23288143 159918 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 316 2 0 3 4.0 CN1CC=C(c2cn(C(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL410710 159918 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 316 2 0 3 4.0 CN1CC=C(c2cn(C(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
24968181 84027 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207378 84027 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44435219 91792 0 None -30 4 Human 5.0 pKi = 5 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL241115 91792 0 None -30 4 Human 5.0 pKi = 5 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
168276831 190139 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 369 3 0 4 4.5 c1ccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)cc1 10.1016/j.ejmech.2022.114329
CHEMBL5173511 190139 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 369 3 0 4 4.5 c1ccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)cc1 10.1016/j.ejmech.2022.114329
118626088 165401 0 None -199 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238124 165401 0 None -199 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
168298474 192719 0 None -245 3 Human 5.0 pKi = 5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 384 8 0 5 3.9 CCOCC(Oc1c(C)cccc1C)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219968 192719 0 None -245 3 Human 5.0 pKi = 5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 384 8 0 5 3.9 CCOCC(Oc1c(C)cccc1C)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
155526651 171174 0 None -45 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4458938 171174 0 None -45 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
164622318 185836 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4867534 185836 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
5 139 72 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5202 139 72 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
CHEMBL39 139 72 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
DB08839 139 72 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
275 3360 9 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3360 9 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3360 9 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3360 9 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
4106 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-5HT -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5HT -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5HT -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5HT -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5HT -7 34 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1238 203174 24 3H-LSD -3 16 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 3H-LSD -3 16 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
4106 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -2 34 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-LSD -4 34 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -4 34 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -4 34 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -4 34 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-LSD -2 34 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -2 34 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -2 34 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -2 34 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1809 134 32 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4106 2502 22 3H-LSD -7 34 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -7 34 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -7 34 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -7 34 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 4153 61 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
103 4153 61 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
None 215943 0 125I-LSD 7 11 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
46780481 107531 20 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
4106 2502 22 3H-LSD -2 34 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -2 34 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -2 34 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -2 34 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 3H-LSD -7 34 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -7 34 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -7 34 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -7 34 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1238 203174 24 3H-LSD -5 16 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 3H-LSD -5 16 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
4106 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1621 2429 17 3H-LSD -17 45 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -17 45 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -17 45 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -17 45 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -17 45 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
4106 2502 22 125I-LSD -4 34 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 125I-LSD -4 34 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 125I-LSD -4 34 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 125I-LSD -4 34 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135398737 958 93 3H-LSD -4 89 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10257 738 31 3H-5HT -39 19 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 31 3H-5HT -39 19 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 31 3H-5HT -39 19 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 31 3H-5HT -39 19 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
282 1419 0 3H-5HT -1122 7 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1419 0 3H-5HT -1122 7 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135 2532 43 3H-5HT -9 58 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-5HT -9 58 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-5HT -9 58 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-5HT -9 58 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-5HT -9 58 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
6450478 216012 0 3H-LSD -2 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
1524 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 125I-LSD -478 52 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1830 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
188 3391 80 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3391 80 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3391 80 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
54841 203127 52 3H-5HT -1 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 52 3H-5HT -1 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 216379 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
3075702 217332 0 3H-LSD -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1220 187 55 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 187 55 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
11957541 1459 40 3H-5HT -2290 16 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1459 40 3H-5HT -2290 16 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1459 40 3H-5HT -2290 16 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1459 40 3H-5HT -2290 16 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1459 40 3H-5HT -2290 16 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
681 1465 72 3H-5HT -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 72 3H-5HT -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 72 3H-5HT -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 72 3H-5HT -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 72 3H-5HT -1995 39 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
107780 1844 54 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 54 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 54 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1524 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 125I-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 3H-LSD -7585 52 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
484 2858 51 3H-5HT -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2858 51 3H-5HT -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2858 51 3H-5HT -24 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
127 3126 52 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 52 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 52 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
119570 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 96 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
243 3202 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 91 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
274 3339 44 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3339 44 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3339 44 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
2402 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 62 3H-LSD -660 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 33 3H-LSD -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
6917970 3691 61 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3691 61 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3691 61 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
2543 3707 68 3H-LSD -218 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3707 68 3H-LSD -194 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-LSD -218 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-LSD -194 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-LSD -218 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-LSD -194 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-LSD -218 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-LSD -194 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-LSD -218 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-LSD -194 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
213 3853 55 3H-LSD -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 55 3H-LSD -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 55 3H-LSD -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 55 3H-LSD -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 55 3H-LSD -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2662 11384 131 3H-LSD -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11384 131 3H-LSD -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
5090 15561 106 3H-LSD -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 3H-LSD -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
10297 27112 30 3H-LSD -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 30 3H-LSD -38 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL146246 38278 0 3H-Lysergic -2754 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 None
156391 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46800 99 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
54477 84653 36 3H-5HT -138 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 3H-5HT -138 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
21830793 91835 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91835 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 94233 100 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94233 100 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 99967 83 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99967 83 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 133521 14 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 14 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167791 24 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 24 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
5280343 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188275 124 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
12016890 190776 6 3H-5HT -16982 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190776 6 3H-5HT -16982 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
3672 192533 136 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 192533 136 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 193615 112 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 193615 112 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 196535 92 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 196535 92 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 200551 115 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 3H-LSD -239 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 203025 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203025 92 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 204687 20 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 20 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 204718 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 204718 17 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
5311189 204841 11 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204841 11 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205341 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 205501 72 3H-LSD -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205501 72 3H-LSD -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205501 72 3H-LSD -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
119607 206203 113 3H-LSD -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206203 113 3H-LSD -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
3337 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
6852400 215937 0 3H-5HT -25118 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 215937 0 3H-5HT -25118 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
165193 215945 0 3H-5HT -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 0 3H-5HT -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 0 3H-5HT -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
None 215993 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
None 216010 0 3H-5HT - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 2 1 2.1 C[N+](C)(C)CCC1=CNC2=C1C=C(C=C2)O None
None 216010 0 3H-LSD - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 2 1 2.1 C[N+](C)(C)CCC1=CNC2=C1C=C(C=C2)O None
None 216011 0 125I-LSD -436 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
104911 216019 0 3H-LSD -41686 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
25137849 216179 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216214 0 3H-LSD -933 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
None 216239 0 3H-LSD -95499 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 216311 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216312 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216315 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 216316 0 3H-LSD -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 0 3H-LSD -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216318 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 0 3H-LSD -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 0 3H-LSD -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216327 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 216328 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216329 0 3H-LSD -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216330 0 3H-LSD -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 216331 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 216389 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 216390 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 216391 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 216392 0 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 216393 0 3H-LSD -1412 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 216394 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 216395 0 3H-LSD -7 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 216489 0 3H-LSD -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1830 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-LSD -13 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1342 35 49 125I-2-iodo LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 35 49 125I-LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 125I-2-iodo LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 125I-LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 125I-2-iodo LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 125I-LSD -45 19 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 125I-LSD -42 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
11954224 215953 0 3H-5HT -181 58 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1353 1911 93 3H-LSD -1047 83 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
265 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
135398737 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 UNDEFINED -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 UNDEFINED -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 UNDEFINED -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 UNDEFINED -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 UNDEFINED -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
122265 1975 0 3H-LSD 1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
273 1975 0 3H-LSD 1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
CHEMBL1191534 1975 0 3H-LSD 1 2 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
135398737 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135409468 2035 69 3H-LSD -4 39 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 3H-LSD -4 39 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 3H-LSD -4 39 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
265 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 125I-LSD 2 3 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
2389 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
10257 738 31 3H-LSD -8 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 31 3H-LSD -8 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 31 3H-LSD -8 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 31 3H-LSD -8 19 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
2389 3331 118 3H-LSD -645 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -645 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -645 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -645 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -645 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
214 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-LSD -81 30 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3331 118 [3H]lysergic acid diethylamide -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 [3H]lysergic acid diethylamide -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 [3H]lysergic acid diethylamide -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 [3H]lysergic acid diethylamide -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 [3H]lysergic acid diethylamide -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2726 919 68 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 215953 0 3H- LSD -141 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 215953 0 3H-LSD -141 58 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
5 139 72 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
134 2514 24 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
135398737 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 125I-LSD -4 89 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1342 35 49 3H-LSD -45 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 49 3H-LSD -45 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 49 3H-LSD -45 19 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
135 2532 43 3H-5HT -22 58 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-5HT -22 58 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-5HT -22 58 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-5HT -22 58 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-5HT -22 58 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
31101 729 40 3H-5HT -181 36 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 40 3H-5HT -181 36 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 40 3H-5HT -181 36 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 40 3H-5HT -181 36 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 40 3H-5HT -181 36 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
None 215946 0 3H-5HT -89 24 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
15387 45822 55 3H-LSD -186 24 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-LSD -186 24 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
3652 4097 79 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 79 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 79 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 79 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 79 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
15387 45822 55 3H-LSD -186 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 45822 55 3H-LSD -186 24 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
2389 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 121 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2337 3256 77 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 2914 112 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 215938 0 125I-LSD -141 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215938 0 125I-LSD -141 21 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
5 139 72 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
277 1301 62 125I-LSD -97 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
277 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 125I-LSD -97 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 125I-LSD -97 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 125I-LSD -97 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 125I-LSD -97 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
277 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 125I-LSD -58 50 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
179 400 115 3H-LSD -134 49 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 3H-LSD -134 49 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 3H-LSD -134 49 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 3H-LSD -134 49 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 3H-LSD -134 49 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
1225 1471 26 125I-LSD -478 22 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 125I-LSD -478 22 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 125I-LSD -478 22 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 125I-LSD -478 22 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 125I-LSD -478 22 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135398737 958 93 3H-LSD -4 89 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3294 2006 111 3H-LSD -87 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -87 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -87 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -87 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -87 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2337 3256 77 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
180 401 56 3H-LSD -99 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -99 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -99 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -99 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -99 40 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
214 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1971 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2274 3173 58 3H-LSD -23 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 3H-LSD -23 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 3H-LSD -23 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 3H-LSD -23 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 3H-LSD -23 31 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1150 3878 121 3H-LSD -20 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 121 3H-LSD -20 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 121 3H-LSD -20 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 121 3H-LSD -20 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1971 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 125I-LSD -29 30 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2274 3173 58 3H-LSD -70 31 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 3H-LSD -70 31 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 3H-LSD -70 31 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 3H-LSD -70 31 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 3H-LSD -70 31 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1613 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5074 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1212 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1613 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -6 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
209 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
277 1301 62 3H-LSD -97 50 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-LSD -97 50 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-LSD -97 50 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-LSD -97 50 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-LSD -97 50 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
16106 118146 34 3H-LSD -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 3H-LSD -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
5 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1150 3878 121 3H-5HT -20 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 121 3H-5HT -20 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 121 3H-5HT -20 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 121 3H-5HT -20 25 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
240 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 944 43 3H-5HT -316 24 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
107780 1844 54 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 54 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 54 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
206 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
2389 3331 118 3H-LSD -2570 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2470 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1712 2492 43 3H-LSD -39 22 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 3H-LSD -39 22 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 3H-LSD -39 22 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 3H-LSD -39 22 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 3H-LSD -39 22 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2470 3653 50 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5074 3332 80 3H-5HT -64 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-5HT -64 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-5HT -64 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-5HT -64 30 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-5HT -91 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
16351 102730 47 3H-LSD -7 6 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL304902 102730 47 3H-LSD -7 6 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
279 1661 26 3H-LSD -3 18 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 26 3H-LSD -3 18 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 26 3H-LSD -3 18 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
1621 2429 17 3H-5HT -17 45 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-5HT -17 45 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-5HT -17 45 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-5HT -17 45 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-5HT -17 45 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
209 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
73333 5963 31 3H-LSD -6 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5963 31 3H-LSD -6 9 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
242 470 124 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
282 1419 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1419 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
242 470 124 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
282 1419 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1419 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135398737 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
209 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
209 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
10090005 215986 0 3H-LSD -21 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
1238 203174 24 3H-LSD -3 16 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 3H-LSD -3 16 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
214 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-LSD -81 30 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
206 2493 16 125I-LSD -1318 25 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2493 16 125I-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 125I-LSD -1318 25 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 125I-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 125I-LSD -1318 25 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 125I-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 3H-LSD -1995 25 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
7153 98020 77 3H-LSD -91 34 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 3H-LSD -91 34 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1209 1658 75 125I-LSD -46 32 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 125I-LSD -46 32 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 125I-LSD -46 32 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 125I-LSD -46 32 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 125I-LSD -46 32 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2337 3256 77 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
107 141 121 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
134 2514 24 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
180 401 56 3H-LSD -154 40 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -154 40 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -154 40 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -154 40 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -154 40 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3294 2006 111 3H-LSD -87 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -87 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -87 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -87 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -87 45 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1809 134 32 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2337 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2726 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135 2532 43 125I-LSD -9 58 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 125I-LSD -9 58 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 125I-LSD -9 58 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 125I-LSD -9 58 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 125I-LSD -9 58 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1427 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 3H-5HT -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
152 364 29 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 364 29 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 364 29 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2389 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2543 3707 68 3H-5HT -954 32 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-5HT -954 32 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-5HT -954 32 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-5HT -954 32 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-5HT -954 32 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4106 2502 22 3H-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-LSD -7 34 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1621 2429 17 3H-LSD -16 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -16 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -16 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -16 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -16 45 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3590 83 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
11954224 215953 0 3H-LSD -181 58 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398745 2914 112 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1238 203174 24 3H-LSD -5 16 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 3H-LSD -5 16 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2429 17 3H-LSD -17 45 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -17 45 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -17 45 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -17 45 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -17 45 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1621 2429 17 3H-LSD -9 45 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -9 45 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -9 45 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -9 45 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -9 45 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
135398737 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-5HT -4 89 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2865 4143 73 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2726 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2389 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3331 118 UNDEFINED -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 UNDEFINED -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 UNDEFINED -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 UNDEFINED -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 UNDEFINED -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11954259 215979 0 3H-LSD -870 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
11954259 215979 0 3H-LSD -870 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
1427 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 2013 54 125I-LSD -19 27 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
130 3500 47 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3500 47 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3500 47 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
242 470 124 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
107 141 121 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2389 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 121 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
7153 98020 77 125I-LSD -125 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 125I-LSD -125 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5 139 72 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
185 4006 60 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 60 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 60 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 60 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2389 3331 118 3H-LSD -2570 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115237 55585 119 3H-LSD -489 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 3H-LSD -489 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
206 2493 16 3H-5HT -16 25 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 3H-5HT -16 25 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 3H-5HT -16 25 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1220 187 55 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 55 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 55 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 55 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3036864 202754 19 125I-LSD -10471 28 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202754 19 125I-LSD -10471 28 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202754 19 125I-LSD -10471 28 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202754 19 125I-LSD -10471 28 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
7153 98020 77 UNDEFINED -125 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 77 UNDEFINED -125 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1809 134 32 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 32 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
134 2514 24 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3707 68 3H-LSD -218 32 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-LSD -218 32 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-LSD -218 32 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-LSD -218 32 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-LSD -218 32 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
133 2496 52 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1613 2348 53 3H-LSD -5 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -5 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -5 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -5 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -5 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2914 112 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
186 1807 52 3H-LSD -457 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1807 52 3H-LSD -457 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1807 52 3H-LSD -457 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
5656 203066 87 3H-5HT 3 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 87 3H-5HT 3 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1212 1662 50 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
274 3339 44 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3339 44 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3339 44 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
1524 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 3H-LSD -269 52 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
279 1661 26 3H-LSD -7 18 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1661 26 3H-LSD -7 18 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1661 26 3H-LSD -7 18 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
4106 2502 22 3H-5HT -7 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5HT -7 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5HT -7 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5HT -7 34 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2105 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
265 128 0 3H-LSD 2 3 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 3H-LSD 2 3 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 3H-LSD 2 3 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
11653679 181191 1 UNDEFINED -44 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 181191 1 UNDEFINED -44 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
11976 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
11976 920 59 3H-LSD -3 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 3H-LSD -3 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 3H-LSD -3 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 3H-LSD -3 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
11976 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 3H-LSD -2 24 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135 2532 43 3H-LSD -9 58 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -9 58 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -9 58 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -9 58 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -9 58 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
107 141 121 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2726 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
133 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 2514 24 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1588 2325 27 3H-5HT -28 44 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-5HT -28 44 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-5HT -28 44 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-5HT -28 44 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-5HT -28 44 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
133 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2105 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1613 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
191 403 98 125I-LSD -7 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 125I-LSD -7 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 125I-LSD -7 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 125I-LSD -7 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 125I-LSD -7 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
135398737 958 93 3H-5HT -4 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-5HT -4 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-5HT -4 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-5HT -4 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-5HT -4 89 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1346 83 117 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
280 83 117 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
9899402 83 117 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
CHEMBL9666 83 117 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
37459 746 13 3H-5HT -74 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 746 13 3H-5HT -74 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 746 13 3H-5HT -74 25 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 958 93 125I-LSD -8 89 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 125I-LSD -8 89 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 125I-LSD -8 89 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 125I-LSD -8 89 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 125I-LSD -8 89 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
133 2496 52 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2496 52 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
5074 3332 80 3H-5HT -91 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-5HT -91 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-5HT -91 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-5HT -91 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
28 3496 46 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3496 46 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3496 46 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1613 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
11954259 215979 0 3H-LSD -870 43 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
31101 729 40 3H-LSD -23 36 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 40 3H-LSD -23 36 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 40 3H-LSD -23 36 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 40 3H-LSD -23 36 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 40 3H-LSD -23 36 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1613 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-LSD -5 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3256 77 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5074 3332 80 3H-LSD -91 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-LSD -91 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-LSD -91 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-LSD -91 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
180 401 56 3H-5HT -154 40 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-5HT -154 40 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-5HT -154 40 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-5HT -154 40 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-5HT -154 40 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
134 2514 24 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1809 134 32 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
145 140 49 3H-LSD -7 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-LSD -7 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-LSD -7 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-LSD -7 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
270 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
6918447 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
CHEMBL80937 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
270 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
6918447 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
CHEMBL80937 2294 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
173 3262 95 3H-LSD -41 23 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 95 3H-LSD -41 23 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 95 3H-LSD -41 23 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1353 1911 93 3H-LSD -1047 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 3H-LSD -2951 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -2951 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -2951 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -2951 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -2951 83 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
134 2514 24 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 24 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1212 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-5HT -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1212 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
107 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1712 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1712 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 3H-LSD -12 22 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
206 2493 16 3H-LSD -1318 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 3H-LSD -1318 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 3H-LSD -1318 25 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
None 216135 0 3H-LSD -4073 24 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
107 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 139 72 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 958 93 3H-5HT -8 89 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-5HT -8 89 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-5HT -8 89 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-5HT -8 89 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-5HT -8 89 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135 2532 43 3H-LSD -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -22 58 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5074 3332 80 3H-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1574 81 60 125I-LSD -4 21 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 125I-LSD -4 21 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 125I-LSD -4 21 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1809 134 32 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
180 401 56 3H-5HT -371 40 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-5HT -371 40 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-5HT -371 40 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-5HT -371 40 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-5HT -371 40 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2477 745 59 3H-5HT -61 29 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 59 3H-5HT -61 29 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 59 3H-5HT -61 29 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 59 3H-5HT -61 29 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 59 3H-5HT -61 29 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 3H-5HT -478 52 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 2514 24 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
None 216450 0 UNDEFINED -26 28 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
2726 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 3H-LSD -4 89 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-LSD -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 958 93 3H-Risperidone -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-Risperidone -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-Risperidone -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-Risperidone -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-Risperidone -4 89 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10257 738 31 3H-5HT -8 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 31 3H-5HT -8 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 31 3H-5HT -8 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 31 3H-5HT -8 19 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
133 2496 52 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2337 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10624 70300 19 3H-LSD -32 33 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70300 19 3H-LSD -32 33 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70300 19 3H-LSD -32 33 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
179 400 115 3H-LSD -134 49 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 3H-LSD -134 49 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 3H-LSD -134 49 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 3H-LSD -134 49 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 3H-LSD -134 49 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
202 1508 77 3H-5HT 1 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 77 3H-5HT 1 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 77 3H-5HT 1 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 77 3H-5HT 1 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 77 3H-5HT 1 30 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
135398745 2914 112 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3294 2006 111 3H-LSD -33 45 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -33 45 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -33 45 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -33 45 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -33 45 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2389 3331 118 3H-Risperidone -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-Risperidone -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-Risperidone -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-Risperidone -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-Risperidone -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 121 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5074 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2389 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -645 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115 3791 80 3H-LSD -10 27 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 80 3H-LSD -10 27 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 80 3H-LSD -10 27 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
24861250 200000 0 UNDEFINED -7 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 None
CHEMBL595252 200000 0 UNDEFINED -7 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 None
1150 3878 121 125I-LSD -7 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3878 121 125I-LSD -20 25 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 121 125I-LSD -7 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 121 125I-LSD -20 25 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 121 125I-LSD -7 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 121 125I-LSD -20 25 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 121 125I-LSD -7 25 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 121 125I-LSD -20 25 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
5074 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 125I-LSD -91 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
11954259 215979 0 3H-LSD -147 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
135 2532 43 125I-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 125I-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 125I-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 125I-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 125I-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1574 81 60 3H-Lysergic 1 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-Lysergic 1 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-Lysergic 1 21 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
4452 2762 19 3H-LSD -1548 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2762 19 3H-LSD -1548 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2762 19 3H-LSD -1548 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
None 216278 0 3H-LSD -5370 12 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
115 3791 80 125I-LSD -12 27 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 80 125I-LSD -12 27 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 80 125I-LSD -12 27 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
141 1427 35 3H-LSD -1 22 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 35 3H-LSD -1 22 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 35 3H-LSD -1 22 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 35 3H-LSD -1 22 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
135398745 2914 112 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5 139 72 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 121 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
176 398 66 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 66 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 66 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 66 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 66 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
66265 94013 15 None 1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 94013 15 None 1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
3397 205488 112 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
CHEMBL806 205488 112 None - 1 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
3117 207841 103 None -5 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207841 103 None -5 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
2543 3707 68 None -194 32 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 None -194 32 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 None -194 32 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 None -194 32 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 None -194 32 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
216239 23795 118 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23795 118 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23795 118 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
1353 1911 93 None -1047 83 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 None -1047 83 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 None -1047 83 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 None -1047 83 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 None -1047 83 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
448537 160250 89 None -35 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 160250 89 None -35 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2812 4779 101 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 101 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1588 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3198 205513 76 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205513 76 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205513 76 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
4189 206922 96 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206922 96 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206922 96 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1588 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-5HT -28 44 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
None 215938 0 3H-5HT -141 21 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
3005573 57440 50 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL1655 57440 50 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 None
2435 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3590 83 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
None 215938 0 3H-5HT -89 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215938 0 3H-5HT -141 21 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1524 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 96 None -269 52 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5656 203066 87 None 3 40 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 87 None 3 40 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
2543 3707 68 None -218 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 None -218 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 None -218 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 None -218 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 None -218 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 55585 119 None -489 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 119 None -489 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1548955 88581 20 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88581 20 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88581 20 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
3561 19077 39 None -3 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 19077 39 None -3 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
2470 3653 50 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1209 1658 75 None -46 32 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 None -46 32 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 None -46 32 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 None -46 32 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 None -46 32 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2470 3653 50 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
73333 5963 31 None -6 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5963 31 None -6 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2247 505 81 None -53 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 None -53 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 None -53 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 None -53 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 None -53 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
4098 32505 30 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32505 30 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32505 30 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
2337 3256 77 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
3042 1414 35 None -51 14 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1414 35 None -51 14 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1414 35 None -51 14 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1414 35 None -51 14 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1414 35 None -51 14 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
2303 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 68 None -346 26 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
2162 41514 100 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
CHEMBL1491 41514 100 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
1201549 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 597 24 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
3652 4097 79 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 79 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 79 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 79 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 79 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1222 1664 49 None -138 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 49 None -138 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 49 None -138 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 49 None -138 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 49 None -138 33 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2286 3183 51 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3183 51 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3183 51 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3183 51 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3183 51 None -26 30 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1016 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3747 78 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
3191 102858 97 None -15 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102858 97 None -15 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
191 403 98 3H-LSD -20 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 3H-LSD -20 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 3H-LSD -20 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 3H-LSD -20 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 3H-LSD -20 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
133 2496 52 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 215953 0 3H-5HT -707 58 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135 2532 43 3H-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -22 58 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1911 93 3H-LSD -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 3H-Risperidone -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-Risperidone -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-Risperidone -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-Risperidone -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-Risperidone -2951 83 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1782 2518 84 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2518 84 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2518 84 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2518 84 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2518 84 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1830 2590 44 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3033769 3281 61 3H-LSD -1380 19 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3281 61 3H-LSD -1380 19 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3281 61 3H-LSD -1380 19 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3281 61 3H-LSD -1380 19 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3281 61 3H-LSD -1380 19 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1577 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3703 110 3H-LSD -275 21 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
185 4006 60 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
185 4006 60 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 60 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 60 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 60 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 60 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 60 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 60 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5567 42802 27 3H-LSD -5495 8 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42802 27 3H-LSD -5495 8 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
54477 84653 36 3H-LSD -69 23 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 3H-LSD -69 23 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
53389 98447 23 3H-LSD -1 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
CHEMBL275707 98447 23 3H-LSD -1 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
33630 178957 99 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178957 99 3H-LSD -891 28 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
None 215987 0 3H-LSD 1 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 342 1 1 5 1.8 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2O)C=C(C=C4)Cl None
None 215988 0 3H-LSD 1 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 334 4 0 3 4.9 C[N+](C)(CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl)[O-] None
1353 1911 93 3H-5HT -346 83 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-5HT -346 83 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-5HT -346 83 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-5HT -346 83 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-5HT -346 83 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
115 3791 80 3H-5HT -12 27 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 80 3H-5HT -12 27 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 80 3H-5HT -12 27 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2726 919 68 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1577 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3703 110 3H-LSD -275 21 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
54477 84653 36 3H-LSD -69 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84653 36 3H-LSD -69 23 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2865 4143 73 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
274 3339 44 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3339 44 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3339 44 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
134 2514 24 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1574 81 60 3H-5HT -1 21 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-5HT -1 21 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-5HT -1 21 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
5074 3332 80 3H-LSD -64 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 80 3H-LSD -64 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 80 3H-LSD -64 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 80 3H-LSD -64 30 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2398 954 62 125I-LSD -6 29 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 62 125I-LSD -6 29 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 62 125I-LSD -6 29 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 62 125I-LSD -6 29 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 62 125I-LSD -6 29 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
1353 1911 93 3H-LSD -1047 83 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135 2532 43 3H-LSD -21 58 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -21 58 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -21 58 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -21 58 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -21 58 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5 139 72 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1613 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1613 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 3H-5HT -6 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1574 81 60 3H-LSD -1 21 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 60 3H-LSD -1 21 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 60 3H-LSD -1 21 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2543 3707 68 3H-LSD -954 32 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 68 3H-LSD -954 32 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 68 3H-LSD -954 32 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 68 3H-LSD -954 32 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 68 3H-LSD -954 32 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
100 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
None 215946 0 3H-LSD -407 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6450478 216012 0 3H-LSD -14 12 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
242 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
124087 1389 114 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1389 114 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1389 114 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1389 114 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1389 114 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
33630 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178957 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
1830 2590 44 None -13 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2590 44 None -13 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2590 44 None -13 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2590 44 None -13 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2590 44 None -13 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
191 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
135398745 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
103 4153 61 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2291 3184 58 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3184 58 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3184 58 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3184 58 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3184 58 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
6075 150108 42 None -13 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 150108 42 None -13 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
1209 1658 75 None -12 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 75 None -12 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 75 None -12 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 75 None -12 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 75 None -12 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
124 2981 47 None -100 33 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 47 None -100 33 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 47 None -100 33 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 47 None -100 33 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 47 None -100 33 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
102 4127 48 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 48 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 48 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 48 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 48 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2585 803 103 None -109 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 803 103 None -109 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 803 103 None -109 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 803 103 None -109 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 803 103 None -109 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
4211 57822 83 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
CHEMBL1670 57822 83 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
5323 202789 103 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 None
CHEMBL62193 202789 103 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 None
2600 3779 74 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3779 74 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3779 74 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3779 74 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3779 74 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1530 2182 50 None -58 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2182 50 None -58 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2182 50 None -58 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2182 50 None -58 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2182 50 None -58 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
4601 206747 35 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 206747 35 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 206747 35 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
135398745 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2351 3286 64 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3286 64 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3286 64 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3286 64 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3286 64 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
107 141 121 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4106 2502 22 3H-5HT -4 34 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 22 3H-5HT -4 34 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 22 3H-5HT -4 34 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 22 3H-5HT -4 34 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
191 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 3H-LSD -7 29 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
100 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
127151 35330 18 None 8 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
3022645 35330 18 None 8 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
CHEMBL14370 35330 18 None 8 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
4011 82408 49 None -28 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 82408 49 None -28 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
202 1508 77 None 1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 77 None 1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 77 None 1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 77 None 1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 77 None 1 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2389 3331 118 None -645 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -645 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -645 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -645 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -645 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 2492 43 None -12 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2492 43 None -12 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2492 43 None -12 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2492 43 None -12 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2492 43 None -12 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 958 93 3H-LSD -8 89 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -8 89 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -8 89 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -8 89 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -8 89 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
4806 4008 88 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 4008 88 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 4008 88 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 4008 88 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 4008 88 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
242 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2514 24 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
100 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3331 118 None -2570 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 None -2570 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 None -2570 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 None -2570 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 None -2570 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1971 2866 38 None -14 30 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 38 None -14 30 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 38 None -14 30 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 38 None -14 30 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 38 None -14 30 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
212 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3806 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
10934 1320 115 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
2955 1320 115 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
782 1320 115 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
CHEMBL1043 1320 115 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
DB00250 1320 115 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
5311507 194815 41 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL53904 194815 41 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 None
5372683 216286 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 C1CN(CCN1CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO None
242 470 124 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
277 1301 62 None -97 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 None -97 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 None -97 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 None -97 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 None -97 50 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
134 2514 24 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
49831411 217746 0 None -1 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
16106 118146 34 None -3 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 None -3 12 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2895 203592 41 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 203592 41 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
214 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 None -81 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2284 3182 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3182 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3182 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3182 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3182 33 None -12 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
277 1301 62 None -58 50 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 None -58 50 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 None -58 50 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 None -58 50 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 None -58 50 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1621 2429 17 3H-LSD -17 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 3H-LSD -17 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 3H-LSD -17 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 3H-LSD -17 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 3H-LSD -17 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6971132 216009 0 3H-LSD -1 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
2274 3173 58 None -23 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 58 None -23 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 58 None -23 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 58 None -23 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 58 None -23 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2398 954 62 None -5 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 62 None -5 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 62 None -5 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 62 None -5 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 62 None -5 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
10090005 215986 0 3H-LSD -8 11 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
1225 1471 26 None -24 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1471 26 None -24 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1471 26 None -24 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1471 26 None -24 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1471 26 None -24 22 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135 2532 43 3H-LSD -22 58 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -22 58 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -22 58 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -22 58 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -22 58 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2865 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1353 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 UNDEFINED -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 UNDEFINED -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 UNDEFINED -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 UNDEFINED -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 UNDEFINED -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
133 2496 52 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2865 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
265 128 0 3H-5HT 2 3 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 3H-5HT 2 3 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 3H-5HT 2 3 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
133 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
3294 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 3653 50 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 50 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 50 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 50 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 50 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
180 401 56 3H-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3294 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 3H-LSD -87 45 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1613 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 125I-LSD -6 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3256 77 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 77 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 77 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 77 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 77 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5 139 72 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
180 401 56 3H-LSD -99 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -99 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -99 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -99 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -99 40 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
214 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3860 58 3H-LSD -79 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 93 3H-LSD -1047 83 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
73333 5963 31 3H-LSD -4 9 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5963 31 3H-LSD -4 9 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
242 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
141 1427 35 3H-LSD -1 22 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 35 3H-LSD -1 22 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 35 3H-LSD -1 22 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 35 3H-LSD -1 22 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
163839 2955 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 2955 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 2955 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
107 141 121 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 121 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 121 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
180 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
180 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 125I-LSD -154 40 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398745 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2914 112 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
180 401 56 None -99 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None -99 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None -99 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None -99 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None -99 40 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398737 958 93 3H-LSD -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16362 3125 71 None -173 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 None -173 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 None -173 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 None -173 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 None -173 30 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135 2532 43 None -21 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -21 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -21 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -21 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -21 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
180 401 56 None -154 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 None -154 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 None -154 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 None -154 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 None -154 40 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
16362 3125 71 None -165 30 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 None -165 30 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 None -165 30 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 None -165 30 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 None -165 30 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
100 3805 58 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
107715 200945 22 None -17 19 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 200945 22 None -17 19 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 200945 22 None -17 19 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
2865 4143 73 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11978813 721 79 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 721 79 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 721 79 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 721 79 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 721 79 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
1588 2325 27 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6761 67799 19 None -9 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67799 19 None -9 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
191 403 98 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1588 2325 27 3H-LSD -21 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 3H-LSD -21 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 3H-LSD -21 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 3H-LSD -21 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 3H-LSD -21 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3294 2006 111 None -87 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 None -87 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 None -87 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 None -87 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 None -87 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3294 2006 111 None -33 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 111 None -33 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 111 None -33 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 111 None -33 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 111 None -33 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
133 2496 52 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135 2532 43 None -22 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 None -22 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 None -22 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 None -22 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 None -22 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3389 217711 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
26987 949 33 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 949 33 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 949 33 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 949 33 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 949 33 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2726 919 68 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1662 50 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
31101 729 40 None -23 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101 729 40 None -22 36 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 40 None -23 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 40 None -22 36 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 40 None -23 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 40 None -22 36 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 40 None -23 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 40 None -22 36 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 40 None -23 36 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 40 None -22 36 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
133 2496 52 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 52 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 52 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 52 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 52 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2105 3054 37 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
209 3057 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
103 4153 61 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
107715 200945 22 None -29 19 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 200945 22 None -29 19 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 200945 22 None -29 19 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
2105 3054 37 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1212 1662 50 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 50 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 50 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 50 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 50 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1613 2348 53 None -6 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None -6 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None -6 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None -6 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None -6 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
209 3057 97 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3057 97 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3057 97 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3057 97 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3057 97 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1613 2348 53 None -5 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 53 None -5 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 53 None -5 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 53 None -5 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 53 None -5 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -4 89 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16106 118146 34 3H-LSD -8 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 118146 34 3H-LSD -8 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
16362 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3125 71 3H-LSD -165 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3125 71 3H-LSD -165 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3125 71 3H-LSD -165 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3125 71 3H-LSD -165 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 3H-LSD -173 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3125 71 3H-LSD -165 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
17676 7072 29 3H-LSD -30 3 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 None
5281082 7072 29 3H-LSD -30 3 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 None
CHEMBL1085 7072 29 3H-LSD -30 3 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 None
180 401 56 3H-LSD -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1809 134 32 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
71299720 215951 0 125I-LSD -588 17 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
101 3822 24 3H-LSD -309 14 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3822 24 3H-LSD -309 14 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3822 24 3H-LSD -309 14 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4143 73 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 73 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 73 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 73 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 73 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1809 134 32 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 32 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 32 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
145 140 49 3H-Lysergic -7 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 3H-Lysergic -7 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 3H-Lysergic -7 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 3H-Lysergic -7 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
242 470 124 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5 139 72 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
145 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 49 125I-LSD -19 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
206 2493 16 3H-5HT -1995 25 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 16 3H-5HT -1995 25 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 16 3H-5HT -1995 25 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
124936 217692 0 3H-LSD -3 7 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 268 3 1 5 4.8 CNC1=CC=C(C=C1)N=NC2=CC3=C(C=C2)N=CS3 None
135398745 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
134551 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 358 27 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
1588 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1588 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 125I-LSD -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
191 403 98 None -7 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 403 98 None -7 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 403 98 None -7 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 403 98 None -7 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 403 98 None -7 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
100 3805 58 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 58 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 58 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 58 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 58 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1588 2325 27 None -21 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 None -21 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 None -21 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 None -21 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 None -21 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3590 83 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 83 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 83 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 83 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 83 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
10531 1420 21 None -21 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1420 21 None -21 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1420 21 None -21 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1420 21 None -21 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1420 21 None -21 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
1588 2325 27 None -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 27 None -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 27 None -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 27 None -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 27 None -28 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
103 4153 61 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 68 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 68 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 68 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 68 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 68 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 None -4 89 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1621 2429 17 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 None -16 45 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11976 920 59 None -3 24 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 920 59 None -3 24 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 920 59 None -3 24 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 920 59 None -3 24 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135398745 2914 112 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 112 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 112 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 112 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954224 215953 0 None -141 58 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 215953 0 None -181 58 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1238 203174 24 None -5 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 203174 24 None -5 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2429 17 None -17 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 17 None -17 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 17 None -17 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 17 None -17 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 17 None -17 45 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1042 1581 23 None -5 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1581 23 None -5 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1581 23 None -5 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1581 23 None -5 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1581 23 None -5 17 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
10531 1420 21 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1420 21 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1420 21 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1420 21 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1420 21 None -9 23 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
103 4153 61 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 61 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 61 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 61 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 61 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
150 2509 21 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2509 21 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2509 21 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2509 21 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2509 21 None -2 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
None 215956 0 125I-LSD -107 6 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
180 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135 2532 43 3H-LSD -21 58 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 43 3H-LSD -21 58 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 43 3H-LSD -21 58 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 43 3H-LSD -21 58 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 43 3H-LSD -21 58 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
180 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-5HT -154 40 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
242 470 124 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 124 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 124 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 124 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 124 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
180 401 56 3H-LSD -371 40 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 56 3H-LSD -371 40 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 56 3H-LSD -371 40 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 56 3H-LSD -371 40 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 56 3H-LSD -371 40 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
46780481 107531 20 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 20 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 20 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 20 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
135409468 2035 69 3H-LSD -3 39 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 69 3H-LSD -3 39 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 69 3H-LSD -3 39 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
135398737 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 93 3H-LSD -4 89 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3337 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
5 139 72 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 72 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 72 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 72 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
101 3822 24 3H-LSD -3981 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3822 24 3H-LSD -3981 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3822 24 3H-LSD -3981 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
277 1301 62 3H-LSD -97 50 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 62 3H-LSD -97 50 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 62 3H-LSD -97 50 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 62 3H-LSD -97 50 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 62 3H-LSD -97 50 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2389 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 118 3H-LSD -2570 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11256720 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
9444 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
CHEMBL1083390 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
DB12680 2055 79 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
4806 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 4008 88 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
242 470 124 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
34 470 124 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
60795 470 124 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
CHEMBL1112 470 124 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
DB01238 470 124 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
275 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
275 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
3246 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
5312144 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL46071 3360 9 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
10337743 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
8429 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
CHEMBL571858 4076 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
3235 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
6918553 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
CHEMBL329383 3520 15 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
3232 3509 19 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
3248571 3509 19 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
CHEMBL60264 3509 19 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
10202564 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
3217 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
CHEMBL362628 1524 14 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
10150497 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
3240 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
CHEMBL392760 4074 47 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
16071605 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
7356 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
CHEMBL2103880 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
DB12229 880 26 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
276 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
5312149 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
CHEMBL431298 3513 50 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
3241 3521 24 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
6918649 3521 24 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
CHEMBL1210710 3521 24 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
21071390 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
8689 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
CHEMBL3286580 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
DB11957 1987 53 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
3337 206367 27 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
179 400 115 None -134 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 115 None -134 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 115 None -134 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 115 None -134 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 115 None -134 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2543 3707 68 None -194 32 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
5358 3707 68 None -194 32 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
54 3707 68 None -194 32 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
CHEMBL128 3707 68 None -194 32 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
DB00669 3707 68 None -194 32 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
206 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
206 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
206 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
68848 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
68848 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
68848 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
CHEMBL12314 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
CHEMBL12314 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
CHEMBL12314 2493 16 None -1995 25 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
152 364 29 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
2107 364 29 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
CHEMBL275854 364 29 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
206 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
206 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
206 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
68848 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
68848 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
68848 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
CHEMBL12314 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
CHEMBL12314 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
CHEMBL12314 2493 16 None -1318 25 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
29 792 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 792 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 792 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
197706 1464 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1464 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1464 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
1355 2011 88 None -158 16 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
142 2011 88 None -158 16 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
CHEMBL478 2011 88 None -158 16 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
DB12110 2011 88 None -158 16 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
2389 3331 118 None -2570 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
5073 3331 118 None -2570 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
96 3331 118 None -2570 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
CHEMBL85 3331 118 None -2570 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
DB00734 3331 118 None -2570 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
2543 3707 68 None -218 32 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
5358 3707 68 None -218 32 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
54 3707 68 None -218 32 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
CHEMBL128 3707 68 None -218 32 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
DB00669 3707 68 None -218 32 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
1209 1658 75 None -46 32 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
203 1658 75 None -46 32 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
3386 1658 75 None -46 32 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
CHEMBL41 1658 75 None -46 32 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
DB00472 1658 75 None -46 32 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
107780 1844 54 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 1844 54 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 1844 54 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
2470 3653 50 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
3300 3653 50 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
5265 3653 50 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
99 3653 50 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
CHEMBL267930 3653 50 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
10 723 28 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 723 28 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 723 28 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3652 4097 79 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4097 79 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4097 79 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4097 79 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4097 79 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
101 3822 24 None -3981 14 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
55752 3822 24 None -3981 14 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
CHEMBL35057 3822 24 None -3981 14 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
1809 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
1809 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
1809 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
4 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
4 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
4 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
CHEMBL18840 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
CHEMBL18840 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
CHEMBL18840 134 32 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
1809 134 32 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
4 134 32 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
CHEMBL18840 134 32 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
109 902 31 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
2689 902 31 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
CHEMBL27403 902 31 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
121930 2396 35 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
18 2396 35 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
CHEMBL1256693 2396 35 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
2389 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
2389 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
5073 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
5073 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
96 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
96 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
CHEMBL85 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
CHEMBL85 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
DB00734 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
DB00734 3331 118 None -645 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
163839 2955 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
268 2955 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
CHEMBL55171 2955 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
108029 3414 57 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
23 3414 57 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
CHEMBL18785 3414 57 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
1150 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
1150 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
125 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
125 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
CHEMBL6640 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
CHEMBL6640 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
DB08653 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
DB08653 3878 121 None -20 25 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
115 3791 80 None -12 27 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
4296 3791 80 None -12 27 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
CHEMBL274866 3791 80 None -12 27 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
202 1508 77 None 1 30 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
60835 1508 77 None 1 30 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
972 1508 77 None 1 30 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
CHEMBL1175 1508 77 None 1 30 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
DB00476 1508 77 None 1 30 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
115 3791 80 None -10 27 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
4296 3791 80 None -10 27 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
CHEMBL274866 3791 80 None -10 27 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
134 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
134 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
134 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
134 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
1775 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
1775 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
1775 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1775 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
9681 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
9681 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
9681 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
9681 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
CHEMBL1065 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
CHEMBL1065 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
CHEMBL1065 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
CHEMBL1065 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
DB00247 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
DB00247 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
DB00247 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
DB00247 2514 24 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
267 1447 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
9847259 1447 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
CHEMBL4214961 1447 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
134 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
134 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
134 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1775 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
1775 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
1775 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
9681 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
9681 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
9681 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
CHEMBL1065 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
CHEMBL1065 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
CHEMBL1065 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
DB00247 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
DB00247 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
DB00247 2514 24 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1574 81 60 None -1 21 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
218 81 60 None -1 21 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
CHEMBL266591 81 60 None -1 21 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
277 1301 62 None -97 50 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
2913 1301 62 None -97 50 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
765 1301 62 None -97 50 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
CHEMBL516 1301 62 None -97 50 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
DB00434 1301 62 None -97 50 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
265 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
265 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
265 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
89576 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
89576 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
89576 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
CHEMBL1288652 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
CHEMBL1288652 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
CHEMBL1288652 128 0 None 2 3 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
180 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
180 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
180 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
200 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
200 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
200 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
2160 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
2160 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
2160 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
CHEMBL629 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
CHEMBL629 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
CHEMBL629 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
DB00321 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
DB00321 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
DB00321 401 56 None -154 40 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
133 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
133 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
133 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
1723 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
1723 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
1723 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
28693 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
28693 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
28693 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
CHEMBL19215 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
CHEMBL19215 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
CHEMBL19215 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
DB13520 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
DB13520 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
DB13520 2496 52 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
145 140 49 None -19 30 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
1832 140 49 None -19 30 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
CHEMBL7257 140 49 None -19 30 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
DB14010 140 49 None -19 30 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
277 1301 62 None -58 50 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
2913 1301 62 None -58 50 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
765 1301 62 None -58 50 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
CHEMBL516 1301 62 None -58 50 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
DB00434 1301 62 None -58 50 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
1342 35 49 None -42 19 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
3 35 49 None -42 19 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
CHEMBL277120 35 49 None -42 19 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
133 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
133 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
133 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
133 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
1723 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
1723 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
1723 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
1723 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
28693 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
28693 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
28693 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
28693 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
CHEMBL19215 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
CHEMBL19215 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
CHEMBL19215 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
CHEMBL19215 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
DB13520 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
DB13520 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
DB13520 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
DB13520 2496 52 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
180 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
180 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
180 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
200 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
200 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
200 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
2160 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
2160 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
2160 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
CHEMBL629 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
CHEMBL629 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
CHEMBL629 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
DB00321 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
DB00321 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
DB00321 401 56 None -99 40 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
135 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
135 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
135 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
1796 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
1796 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
1796 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
4184 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
4184 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
4184 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
CHEMBL6437 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
CHEMBL6437 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
CHEMBL6437 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
DB06148 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
DB06148 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
DB06148 2532 43 None -21 58 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
209 3057 97 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
2113 3057 97 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
4748 3057 97 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
CHEMBL567 3057 97 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
DB00850 3057 97 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
101 3822 24 None -309 14 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
55752 3822 24 None -309 14 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
CHEMBL35057 3822 24 None -309 14 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
5074 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
5074 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
5074 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
5074 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
97 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
97 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
97 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
97 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
CHEMBL267777 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
CHEMBL267777 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
CHEMBL267777 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
CHEMBL267777 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
DB12693 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
DB12693 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
DB12693 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
DB12693 3332 80 None -91 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
5 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
5 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
5 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5202 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
5202 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
5202 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
CHEMBL39 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
CHEMBL39 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
CHEMBL39 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
DB08839 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
DB08839 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
DB08839 139 72 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
135 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
135 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
135 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
1796 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
1796 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
1796 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
4184 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
4184 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
4184 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
CHEMBL6437 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
CHEMBL6437 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
CHEMBL6437 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
DB06148 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
DB06148 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
DB06148 2532 43 None -22 58 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
5074 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
5074 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
5074 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
97 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
97 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
97 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
CHEMBL267777 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
CHEMBL267777 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
CHEMBL267777 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
DB12693 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
DB12693 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
DB12693 3332 80 None -64 30 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
278 1418 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
3065 1418 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
CHEMBL1967279 1418 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
141 1427 35 None -1 22 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
6089 1427 35 None -1 22 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
CHEMBL12420 1427 35 None -1 22 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
DB01488 1427 35 None -1 22 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
3294 2006 111 None -87 45 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
71360 2006 111 None -87 45 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
87 2006 111 None -87 45 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
CHEMBL14376 2006 111 None -87 45 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
DB04946 2006 111 None -87 45 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
16362 3125 71 None -165 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
2172 3125 71 None -165 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
90 3125 71 None -165 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
CHEMBL1423 3125 71 None -165 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
DB01100 3125 71 None -165 30 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
100 3805 58 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
2637 3805 58 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
5452 3805 58 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
CHEMBL479 3805 58 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
DB00679 3805 58 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
5 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
5 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
5202 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
5202 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5202 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5202 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
CHEMBL39 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
CHEMBL39 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
CHEMBL39 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
CHEMBL39 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
DB08839 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
DB08839 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
DB08839 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
DB08839 139 72 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
134551 358 27 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
271 358 27 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
885 358 27 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
CHEMBL1403281 358 27 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
191 403 98 None -20 29 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
201 403 98 None -20 29 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
2170 403 98 None -20 29 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
CHEMBL1113 403 98 None -20 29 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
DB00543 403 98 None -20 29 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
1212 1662 50 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
204 1662 50 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
3372 1662 50 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
CHEMBL726 1662 50 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
DB00623 1662 50 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
279 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
279 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
49381 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
49381 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
CHEMBL63756 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
CHEMBL63756 1661 26 None -7 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
107 141 121 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
1833 141 121 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
CHEMBL8165 141 121 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
3294 2006 111 None -33 45 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
71360 2006 111 None -33 45 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
87 2006 111 None -33 45 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
CHEMBL14376 2006 111 None -33 45 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
DB04946 2006 111 None -33 45 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
270 2294 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
6918447 2294 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
CHEMBL80937 2294 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
1613 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
1613 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
205 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
205 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
3964 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
3964 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
CHEMBL831 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
CHEMBL831 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
DB00408 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
DB00408 2348 53 None -6 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
1613 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
1613 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
205 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
205 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
3964 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
3964 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
CHEMBL831 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
CHEMBL831 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
DB00408 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
DB00408 2348 53 None -5 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
274 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
274 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
5312145 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
5312145 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL433461 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL433461 3339 44 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
31101 729 40 None -23 36 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
31101 729 40 None -22 36 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
35 729 40 None -23 36 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
35 729 40 None -22 36 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
403 729 40 None -23 36 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
403 729 40 None -22 36 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
CHEMBL493 729 40 None -23 36 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
CHEMBL493 729 40 None -22 36 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
DB01200 729 40 None -23 36 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
DB01200 729 40 None -22 36 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
2105 3054 37 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
47811 3054 37 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
48 3054 37 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
CHEMBL531 3054 37 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
DB01186 3054 37 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
274 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
274 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
5312145 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
5312145 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL433461 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL433461 3339 44 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
167 3431 0 None -25 5 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
9821498 3431 0 None -25 5 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
107 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
107 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
107 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
1833 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
1833 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
1833 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
CHEMBL8165 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
CHEMBL8165 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
CHEMBL8165 141 121 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
10257 738 31 None -8 19 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
144 738 31 None -8 19 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
CHEMBL416526 738 31 None -8 19 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
DB01445 738 31 None -8 19 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
6918515 2612 38 None 4 7 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
71 2612 38 None 4 7 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
CHEMBL7318 2612 38 None 4 7 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
2726 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2726 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
621 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
621 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
83 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
83 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
CHEMBL71 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
CHEMBL71 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
DB00477 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
DB00477 919 68 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
1043 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
1043 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
1043 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
149 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
149 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
149 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
8223 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
8223 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
8223 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
CHEMBL442 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
CHEMBL442 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
CHEMBL442 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
DB00696 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
DB00696 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
DB00696 1582 14 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
10171 56 18 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
272 56 18 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
CHEMBL274384 56 18 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
12 1553 17 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918513 1553 17 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
CHEMBL267615 1553 17 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
279 1661 26 None -3 18 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
49381 1661 26 None -3 18 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
CHEMBL63756 1661 26 None -3 18 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
1212 1662 50 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
204 1662 50 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
3372 1662 50 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
CHEMBL726 1662 50 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
DB00623 1662 50 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
209 3057 97 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
2113 3057 97 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
4748 3057 97 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
CHEMBL567 3057 97 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
DB00850 3057 97 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
191 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
191 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
201 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
201 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
2170 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
2170 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
CHEMBL1113 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
CHEMBL1113 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
DB00543 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
DB00543 403 98 None -7 29 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
1588 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
1588 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
1588 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
1588 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
28864 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
28864 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
28864 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
28864 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
43 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
43 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
43 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
43 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
CHEMBL157138 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
CHEMBL157138 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
CHEMBL157138 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL157138 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
DB00589 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
DB00589 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
DB00589 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB00589 2325 27 None -28 44 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
275 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
275 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
3246 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
5312144 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL46071 3360 9 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
135398737 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
38 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
722 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
CHEMBL42 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
DB00363 958 93 None -4 89 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
135398737 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
135398737 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
135398737 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
135398737 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
38 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
38 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
38 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
38 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
722 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
722 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
722 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
722 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
CHEMBL42 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
CHEMBL42 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
CHEMBL42 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
CHEMBL42 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
DB00363 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
DB00363 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
DB00363 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
DB00363 958 93 None -4 89 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
122265 1975 0 None 1 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
273 1975 0 None 1 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
CHEMBL1191534 1975 0 None 1 2 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
135398745 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
135398745 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
47 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
47 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
CHEMBL715 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
DB00334 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
DB00334 2914 112 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
1588 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
1588 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
28864 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
28864 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
43 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
43 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL157138 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
CHEMBL157138 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB00589 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
DB00589 2325 27 None -21 44 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
135398745 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
135398745 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
47 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
47 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
CHEMBL715 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
CHEMBL715 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
DB00334 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
DB00334 2914 112 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
10531 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
10531 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
121 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
121 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
888 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
888 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
CHEMBL1732 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
CHEMBL1732 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
DB00320 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
DB00320 1420 21 None -21 23 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
100 3805 58 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
2637 3805 58 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
5452 3805 58 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
CHEMBL479 3805 58 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
DB00679 3805 58 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
1621 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
1621 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
17 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
17 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
5761 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
5761 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL263881 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
CHEMBL263881 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB04829 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
DB04829 2429 17 None -17 45 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
1043 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
1043 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
149 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
149 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
8223 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
8223 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
CHEMBL442 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
CHEMBL442 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
DB00696 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
DB00696 1582 14 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
103 4153 61 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2875 4153 61 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
5736 4153 61 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
CHEMBL285802 4153 61 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
DB09225 4153 61 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2726 919 68 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
621 919 68 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
83 919 68 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
CHEMBL71 919 68 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
DB00477 919 68 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
1621 2429 17 None -16 45 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
17 2429 17 None -16 45 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
5761 2429 17 None -16 45 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL263881 2429 17 None -16 45 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB04829 2429 17 None -16 45 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
4106 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
4106 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
4106 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
4106 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
5358812 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
5358812 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
5358812 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
5358812 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
89 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
89 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
89 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
89 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
CHEMBL93240 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
CHEMBL93240 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
CHEMBL93240 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
CHEMBL93240 2502 22 None -7 34 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
4106 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
4106 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
4106 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
5358812 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
5358812 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
5358812 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
89 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
89 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
89 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
CHEMBL93240 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
CHEMBL93240 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
CHEMBL93240 2502 22 None -2 34 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
103 4153 61 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
2875 4153 61 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
5736 4153 61 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
CHEMBL285802 4153 61 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
DB09225 4153 61 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055